NPS-2143(NPS 2143; SB 262470A ) is a selective potent calcium ion-sensing receptor antagonist with IC50 of 43 and 41 nM for cytoplasmic Ca2+ concentrations and parathyroid hormone secretion, respectively.NPS-2143(NPS 2143; SB 262470A ) is useful for treatment of osteoporosis
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
2014年7月24日星期四
PI3K/Akt/mTOR|from medchemexpress
The PI3K/Akt/mTOR pathway is a prototypic survival pathway that is constitutively activated in many types of cancer. Mechanisms for pathway activation include loss of tumor suppressor PTEN function, amplification or mutation of PI3K, amplification or mutation of Akt, activation of growth factor receptors, and exposure to carcinogens. Once activated, signaling through Akt can be propagated to a diverse array of substrates, including mTOR, a key regulator of protein translation. This pathway is an attractive therapeutic target in cancer because it serves as a convergence point for many growth stimuli, and through its downstream substrates, controls cellular processes that contribute to the initiation and maintenance of cancer. Moreover, activation of the Akt/mTOR pathway confers resistance to many types of cancer therapy, and is a poor prognostic factor for many types of cancers.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
CDK inhibitor,high quality inhibitors from medchemexpress
Cdk Inhibitors
medchemexpress now offer thousands of Cdk Inhibitors. Cell cycle progression is controlled, in part, by a family of cyclin-dependent kinases (Cdks) that work to phosphorylate key substrates involved in each phase of cell cycle progression. Cdks are the catalytic subunits of serine/threonine protein kinases. Phosphorylation events play a key role in the regulation of these proteins. Cdk Inhibitors offered by Santa Cruz inhibit Cdk and, in some cases, other phosphorylation and serine/threonine protein kinase related proteins. View detailed Cdk Inhibitor specifications, including Cdk Inhibitor CAS number, molecular weight, molecular formula and chemical structure, by linking to the specific product blocks.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
VX-745|cas 209410-46-8|medchemexpress
VX-745 ,cas:209410-46-8 is highly potent and selective p38α inhibitor (IC50 = 10 nM). VX-745 also blocks TNFα production in LPS-stimulated HWB in vitro (IC50 = 177 nM). VX-745 displays 1000-fold selectivity over closely related kinases, including ERK1, MK2 and JNK1-3. VX-745 is a lead anti-inflammatory candidate, p38 MAPK inhibitor (IC50=10 nM) for the treatment of Rheumatoid arthritis (RA).
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
GS-9973|CAS No1229208-44-9|medchemexpress
GS-9973 also known GS9973; GS 9973, cas no:1229208-44-9 is a highly selective and orally efficacious Syk inhibitor(IC50= 7.7 nM) which is currently undergoing clinical evaluation for autoimmune and oncology indications.
IC50 value: 7.7 nM [1]
Target: Syk
The most advanced Syk inhibitor, R406, 1 (or its prodrug form fostamatinib, 2), has shown efficacy in multiple therapeutic indications, but its clinical progress has been hampered by dose-limiting adverse effects that have been attributed, at least in part, to the off-target activities of 1. It is expected that GS-9973 is a more selective Syk inhibitor would provide a greater therapeutic window.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
IC50 value: 7.7 nM [1]
Target: Syk
The most advanced Syk inhibitor, R406, 1 (or its prodrug form fostamatinib, 2), has shown efficacy in multiple therapeutic indications, but its clinical progress has been hampered by dose-limiting adverse effects that have been attributed, at least in part, to the off-target activities of 1. It is expected that GS-9973 is a more selective Syk inhibitor would provide a greater therapeutic window.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
SU5416|Semaxinib|204005-46-9| from medchemexpress
SU5416 (Semaxinib), cas NO.204005-46-9,a VEGF receptor inhibitor and an aryl hydrocarbon receptor (AHR) agonist, represents a new alternative for immunomodulation. SU5416 went as far as Phase III clinical trials as an anticancer agent, putatively because of its activity as a VEGFR-2 inhibitor. SU5416 has biologic activity in patients with refractory acute myeloid leukemia or myelodysplastic syndromes. SU5416 inhibits tumor vascularization and growth of multiple tumor types.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
2014年7月22日星期二
where can you buy inhibitors for your research?
you must hear of medchemexpress.<http://www.medchemexpress.com>
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
MCE chemists are highly experienced in preparing biologically active molecules that are both structurally and synthetically diverse. The volume of our products ranges from milligrams to kilograms scale. With rich experiences in customized chemical synthesis, we ensure on-time delivery of diversified compounds to meet all clients’ different requirements.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
MCE chemists are highly experienced in preparing biologically active molecules that are both structurally and synthetically diverse. The volume of our products ranges from milligrams to kilograms scale. With rich experiences in customized chemical synthesis, we ensure on-time delivery of diversified compounds to meet all clients’ different requirements.
Semagacestat | (LY450139) medchemexpress
Semagacestat (LY450139) is a γ-secretase blocker with an IC50 of 15 nM. In treatment of Alzheimer's Disease.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.cas:425386-60-3.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.cas:425386-60-3.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
Topiroxostat(FYX-051) | medchemexpress
Topiroxostat(FYX-051) ,cas:425386-60-3 is a novel and potent xanthine oxidoreductase (XOR) inhibitor with IC50 value of 5.3 nM.
IC50 value: 5.3 nM [1]
Target: xanthine oxidoreductase
in vitro: Steady-state kinetics study showed that FYX-051 initially behaved as a competitive-type inhibitor with a K(i) value of 5.7 × 10(-9) M, then after a few minutes it formed a tight complex with XOR via a Mo-oxygen-carbon atom covalent linkage, as reported previously [3].
in vivo: FYX-051 exhibited a weak CYP3A4-inhibitory activity (18.6%); its Cmax and bioavailability were as high as 4.62 μg/mL (3 mg/kg) and 69.6%, respectively. Moreover, the t1/2 value of 39 was greater (19.7 h) than that of compound 2 (0.97 h) [1]. In the mechanistic study by 52-week oral treatment with topiroxostat at 3 mg/kg to F344 male rats, with and without citrate, simple and papillary transitional cell hyperplasias of the urinary bladder epithelium were observed in 5/17 in the topiroxostat-alone treatment group, along with xanthine-induced nephropathy, in contrast to neither xanthine crystals nor lesions in urinary organs by co-treatment group with citrate [2].
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
IC50 value: 5.3 nM [1]
Target: xanthine oxidoreductase
in vitro: Steady-state kinetics study showed that FYX-051 initially behaved as a competitive-type inhibitor with a K(i) value of 5.7 × 10(-9) M, then after a few minutes it formed a tight complex with XOR via a Mo-oxygen-carbon atom covalent linkage, as reported previously [3].
in vivo: FYX-051 exhibited a weak CYP3A4-inhibitory activity (18.6%); its Cmax and bioavailability were as high as 4.62 μg/mL (3 mg/kg) and 69.6%, respectively. Moreover, the t1/2 value of 39 was greater (19.7 h) than that of compound 2 (0.97 h) [1]. In the mechanistic study by 52-week oral treatment with topiroxostat at 3 mg/kg to F344 male rats, with and without citrate, simple and papillary transitional cell hyperplasias of the urinary bladder epithelium were observed in 5/17 in the topiroxostat-alone treatment group, along with xanthine-induced nephropathy, in contrast to neither xanthine crystals nor lesions in urinary organs by co-treatment group with citrate [2].
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
E 2012 | medchemexpress
E 2012 is γ-secretase inhibitor.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
| CAS No | 870843-42-8 |
|---|
2014年7月21日星期一
MK-0752 | medchemexpress
MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
RO4929097 |medchemexpress
RO4929097 is an orally bioavailable, small-molecule gamma secretase (GS) inhibitor with an IC50 of 4 nM. It binds to GS and blocks activation of Notch receptors, which may inhibit tumor cell proliferation. RO4929097 inhibits Notch processing in tumor cells as measured by the reduction of intracellular Notch expression by Western blot. This leads to reduced expression of the Notch transcriptional target gene Hes 1. RO4929097 does not block tumor cell proliferation or induce apoptosis but instead produces a less transformed, flattened, slower-growing phenotype.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
DAPT | medchemexpress
DAPT(GSI-IX) is inhibitor of γ-secretase. DAPT causes a reduction in Aβ40 and Aβ42 levels in human primary neuronal cultures (IC50 values are 115 and 200 nM for total Aβ and Aβ42 respectively) and in brain extract, cerebrospinal fluid and plasma in vivo. Does not effect APPα and APPβ levels. DAPT blocks Notch signaling in hybrid human-mouse fetal thymus organ culture (FTOC). Activity causes neural cells to commit to neuronal differentiation.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
2014年7月20日星期日
ABC294640 |medchemexpress
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ABC294640 is an orally available, aryladamantane compound and selective inhibitor of sphingosine kinase-2 (SK2) with potential antineoplastic activity. Upon administration, ABC294640 competitively binds to and inhibits SK2, thereby preventing the phosphorylation of the pro-apoptotic amino alcohol sphingosine to sphingosine 1-phosphate (S1P), the lipid mediator that is pro-survival and critical for immunomodulation. This may eventually lead to the induction of apoptosis and may result in an inhibition of cell proliferation in cancer cells overexpressing SK2. SK2 and its isoenzyme SK1 are overexpressed in numerous cancer cell types.
TG 100572 | medchemexpress
TG 100572 is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kinases with IC50 values of 2/7/2/1/0.5 nM for VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse respectively.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
TG 100801 | medchemexpress
TG 100801 is currently in a clinical trial as a first in class, VEGFr2 targeting, topically applied compound for the treatment of AMD. The formation of new blood vessels (angiogenesis), blood vessel leakage, and inflammation contribute to the progression of the eye disease, age-related macular degeneration (AMD), which is the leading cause of irreversible, severe loss of vision in people 55 years of age and older in the developed world. TG100801 is a new drug that inhibits ocular angiogenesis, vascular leak, and inflammation in laboratory studies, and may have great utility in the treatment of diseases such as AMD.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
Saracatinib supplier medchemexpress
Saracatinib (AZD0530) is a highly selective, orally available, dual-specific Src/Abl kinase inhibitor with IC50 of 2.7 and 30 nM for c-Src and Abl kinase, respectively.Saracatinib (AZD0530) is a selective, oral Src inhibitor that has demonstrated antitumour activity in preclinical studies. Methods This open-label, dose-escalation, phase I study evaluated the safety and tolerability of saracatinib in Japanese patients with advanced solid tumours (clinicaltrials.gov NCT00704366). Patients received continuous once-daily oral dosing with saracatinib starting 7 days after a single dose in ascending dose cohorts until dose-limiting toxicity (DLT) or disease progression. Pharmacokinetics and efficacy were also evaluated. Results A total of 12 patients received saracatinib at doses of 50 (n?=?3), 125 (n?=?6), and 175 mg (n?=?3). Median durations of exposure were 65, 44, and 16 days in the 50, 125, and 175 mg cohorts, respectively. The most common adverse events were diarrhoea (67?%), nausea (67?%), decreased appetite (58?%), lymphopenia (50?%) and pyrexia (50?%). The most common grade ≥3 adverse events were leukopenia, lymphopenia, neutropenia, and haemoglobin decreased (all 17?%). DLTs occurred in two patients, both in the 175 mg cohort: grade 3 aspartate aminotransferase increased with grade 3 gamma-glutamyltransferase increased (n?=?1); and grade 3 hypoxia (n?=?1). Following a single dose, saracatinib median t(max) across the doses was 2-4 h, and thereafter plasma concentrations declined in a biphasic manner, with mean terminal half-life of approximately 45 h. Geometric mean saracatinib exposures were 0.8-2.1 times greater than those reported in Caucasian patients. The best response was stable disease (50 mg, n?=?2; 125 mg, n?=?1). Conclusions Saracatinib was tolerated in Japanese patients with advanced solid tumours at doses up to 125 mg.
medchemexpress,provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
medchemexpress,provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
2014年7月17日星期四
Apoptosis |medchemexpress
The cells in the human body is doomed to death, some deaths are physical in nature, some deaths are pathological, research on cell death, has become a hot biology, medical research. People have been known to cell death are at least two ways, namely cell necrosis and apoptosis (apoptosis). Cell necrosis has long been recognized that a cell death, apoptosis and cell death is a way of gradually being recognized.
Apoptosis is a fundamental biological phenomenon cells play essential roles in multicellular organisms eliminate unwanted or abnormal cells. It plays an important role in the evolution and development of the organism, and the environment within which the plurality of system stability. Apoptosis is not only a special type of cell death, but also has important biological significance and complexity of the molecular mechanisms.
Apoptosis is a carefully controlled process of multiple genes. These genes are highly conserved between species, such as Bcl-2 family, caspase family of oncogenes such as C-myc, tumor suppressor gene P53, etc. With the development of molecular biology techniques for a variety of apoptotic process has considerable knowledge, but so far the exact mechanism of apoptosis is not fully understood. The disordered apoptosis may have a direct or indirect relationship with the occurrence of many diseases. Such as cancer, autoimmune diseases, can induce apoptosis of many factors, such as radiation, drugs.
Part of the physical structure of a natural person apoptosis, such as human tail phase, the tail automatically apoptosis during development.
the specialized technician from famous inhibitors supplier Medchemexpresschemicals will tell people main functions of this kind of inhibitors.you can find more information from it.
here are some information about medchemexpress.
Medchemexpress provides thousands of
inhibitors, modulators and agonists with high purity and quality. They also
have excellent customer reviews, precise and professional product citations, tech
support and prompt delivery
Contact:
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Antibody-drug conjugates/ADCs Related |medchemexpress
Now,
let the specialized technician from famous inhibitors supplier Medchemexpress chemicals will tell people main functions
of this kind of inhibitors.
Conjugation to cytotoxic drugs or radionuclides can expand the utility of mAbs and improve their potency and effectiveness, the antibodies are thus used as a means to target and delivery a toxic payload to the selected diseased tissue. This approach is currently a major focus of therapeutic research. Antibodies have been conjugated to a number of cytotoxic drugs, though various linker chemistries and these antibody drug conjugates (ADCs) have the ability to selectively and potently kill antigen–expressing tumor cells in vitro and in xenograft studies. ADCs have demonstrated success in the clinic, and there are now two such drugs, ado-trastuzumab emtansine (Kadcyla®) and brentuximab vedotin (Adcetris®), marketed in the United States. With over 30 ADCs currently undergoing clinical studies, it is likely that more conjugates will be approved in the future.
ADC development has been an iterative learning process, with ADCs evolving from murine antibodies that were conjugated to standard chemotherapeutic drugs to fully human antibodies conjugated to highly potent cytotoxic drugs. Our understanding of ADCs has improved substantially over the past 10 years and we now understand many of the critical factors required for their successful development, including target antigen selection, antibody, linker, and payload. One area of research that has seen recent advancement is that of conjugation chemistry. The implementation of site-specific conjugation, in which conjugation occurs only at engineered cysteine residues or unnatural amino acids for example, has resulted in homogeneous ADC production and improved ADC pharmacokinetic (PK) properties.
About Medchemexpress Chemicals
Medchemexpress provides thousands of
inhibitors, modulators and agonists with high purity and quality. They also
have excellent customer reviews, precise and professional product citations, tech
support and prompt delivery
Contact:
ADDRESS:
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TEL:
609-228-6898
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WEB：www.medchemexpress.com
Anti-infection |medchemexpress
What
is the main function of the cell signaling inhibitors? This should be a very
professional problem. In a word, the professional problem needs to be solved by
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people main functions of this kind of inhibitors.today we will introduce you some information about Anti-infection.
Infection is the invasion of a host organism's bodily tissues by disease-causing organisms, their multiplication, and the reaction of host tissues to these organisms and the toxins they produce. Infectious diseases, also known as transmissible diseases or communicable diseases, comprise clinically evident illness (i.e., characteristic medical signs and/or symptoms of disease) resulting from the infection, presence and growth of pathogenic biological agents in an individual host organism. Infections are caused by infectious agents such as viruses, viroids, and prions, microorganisms such as bacteria, nematodes such as roundworms and pinworms, arthropods such as ticks, mites, fleas, and lice, fungi such as ringworm, and other macroparasites such as tapeworms.
Antiviral drugs are a class of medication used specifically for treating viral infections. Like antibiotics for bacteria, specific antivirals are used for specific viruses. Unlike most antibiotics, antiviral drugs do not destroy their target pathogen; instead they inhibit their development. Antiviral drugs are one class of antimicrobials, a larger group which also includes antibiotic (also termed antibacterial), antifungal and antiparasitic drugs. They are relatively harmless to the host, and therefore can be used to treat infections. They should be distinguished from viricides, which are not medication but deactivate or destroy virus particles, either inside or outside the body. Antivirals also can be found in essential oils of some herbs, such as eucalyptus oil and its constituents.
2014年7月9日星期三
PF-3084014
PF-3084014 is a novel gamma-secretase inhibitor that reduces amyloid-beta (Abeta) production with an in vitro IC(50) of 1.2 nM (whole-cell assay) to 6.2 nM (cell-free assay).
in vitro: The ability of PF-03084014 to inhibit gamma-secretase activity was shown by the reduction of endogenous NICD levels and by the downregulation of Notch target genes Hes-1 and c-Myc in the T-cell acute lymphoblastic leukemia (T-ALL) cell line HPB-ALL. PF-03084014 caused cell growth inhibition of several T-ALL cell lines via cell cycle arrest and induction of apoptosis [1]. PF-03084014 exhibited activity against tumor cell migration, endothelial cell tube formation, and mammosphere formation [3].
in vivo: Guinea pigs were dosed with PF-3084014 for 5 days via osmotic minipump at 0.03 to 3 mg/kg/day and exhibited dose-dependent reduction in brain, CSF, and plasma Abeta. To further characterize Abeta dynamics in brain, CSF, and plasma in relation to drug exposure and Notch-related toxicities, guinea pigs were dosed with 0.03 to 10 mg/kg PF-3084014, and tissues were collected at regular intervals from 0.75 to 30 h after dose. Brain, CSF, and plasma all exhibited dose-dependent reductions in Abeta, and the magnitude and duration of Abeta lowering exceeded those of the reductions in B-cell endpoints [2]. PF-03084014 treatment displayed significant antitumor activity in 10 of the 18 breast xenograft models. However, the antitumor efficacy in most models did not correlate with the in vitro antiproliferation results in the corresponding cell lines, suggesting the critical involvement of tumor microenvironment during Notch activation. In the tested breast xenograft models, the baseline expressions of the Notch receptors, ligands, and the cleaved Notch1 failed to predict the antitumor response to PF-03084014, whereas several Notch pathway target genes, including HEY2, HES4, and HES3, strongly corresponded with the response with a P value less than 0.01. Many of the best molecular predictors of response were also significantly modulated following PF-03084014 treatment you can buy it from medchemexpress.
in vitro: The ability of PF-03084014 to inhibit gamma-secretase activity was shown by the reduction of endogenous NICD levels and by the downregulation of Notch target genes Hes-1 and c-Myc in the T-cell acute lymphoblastic leukemia (T-ALL) cell line HPB-ALL. PF-03084014 caused cell growth inhibition of several T-ALL cell lines via cell cycle arrest and induction of apoptosis [1]. PF-03084014 exhibited activity against tumor cell migration, endothelial cell tube formation, and mammosphere formation [3].
in vivo: Guinea pigs were dosed with PF-3084014 for 5 days via osmotic minipump at 0.03 to 3 mg/kg/day and exhibited dose-dependent reduction in brain, CSF, and plasma Abeta. To further characterize Abeta dynamics in brain, CSF, and plasma in relation to drug exposure and Notch-related toxicities, guinea pigs were dosed with 0.03 to 10 mg/kg PF-3084014, and tissues were collected at regular intervals from 0.75 to 30 h after dose. Brain, CSF, and plasma all exhibited dose-dependent reductions in Abeta, and the magnitude and duration of Abeta lowering exceeded those of the reductions in B-cell endpoints [2]. PF-03084014 treatment displayed significant antitumor activity in 10 of the 18 breast xenograft models. However, the antitumor efficacy in most models did not correlate with the in vitro antiproliferation results in the corresponding cell lines, suggesting the critical involvement of tumor microenvironment during Notch activation. In the tested breast xenograft models, the baseline expressions of the Notch receptors, ligands, and the cleaved Notch1 failed to predict the antitumor response to PF-03084014, whereas several Notch pathway target genes, including HEY2, HES4, and HES3, strongly corresponded with the response with a P value less than 0.01. Many of the best molecular predictors of response were also significantly modulated following PF-03084014 treatment you can buy it from medchemexpress.
LY-411575
LY411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch clevage with withIC50 of 0.39 nM.LY-411575 inhibits γ-secretase which can be assessed by the substrates like amyloid precursor protein (APP) and Notch S3 cleavage [1]. LY-411575, which blocks Notch activation, results in apoptosis in primary and immortalized KS cells [2].you can buy it from medchemexpress.
BMS-708163
BMS-708163 is a gamma-secretase inhibitor that is being developed for the treatment of Alzheimer's disease. Several LC-MS/MS methods have been developed for the determination of BMS-708163 in both plasma and cerebrospinal fluid in support of dog, rat, mouse and human studies. To support non-clinical studies, an LC-MS/MS method with a lower limit of quantitation (LLOQ) of 5 ng/mL, was developed and validated in dog, rat, and mouse plasma by using the deprotonated ion as the precursor ion. To support clinical studies, an LC-MS/MS method with LLOQ of 0.1 ng/mL, was developed and validated in human plasma by using the formate adduct as the precursor ion. Formic acid (0.01%) in water and acetonitrile was found to be the most favorable mobile phases for both deprotonated and formate adduct ions in negative electrospray ionization mode. A combination of a 3M Empore C18 plate for SPE and a Waters Atlantis dC18 analytical column for separation was used to achieve a highly selective solid phase extraction and chromatographic procedure from plasma without dry down and reconstitution steps. In the development of an assay for BMS-708163 in cerebral spinal fluid (CSF), significant non-specific binding of BMS-708163 was observed and resolved with pre- or post-spike of 0.2% Tween 20 into CSF samples. A dilute-and-shoot LC-MS/MS method with LLOQ of 0.1 ng/mL was developed and validated to assess BMS-708163 exposure in human CSF.
2 . Hartley RF, Huang Y, Cassidy M, Razler TM, Qian F, Hussain MA.Degradation kinetics and mechanism of an oxadiazole derivative, design of a stable drug product for BMS-708163, a γ-secretase inhibitor drug candidate.J Pharm Sci. 2012 Sep;101(9):3124-33
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2 . Hartley RF, Huang Y, Cassidy M, Razler TM, Qian F, Hussain MA.Degradation kinetics and mechanism of an oxadiazole derivative, design of a stable drug product for BMS-708163, a γ-secretase inhibitor drug candidate.J Pharm Sci. 2012 Sep;101(9):3124-33
you can it from medchemexpress,best price ,high quality inhibitors!
BMS 299897
BMS-299897 markedly reduced both brain and plasma Abeta in APP-YAC mice with ED(50) values of 86 and 22 mg/kg per os (po), respectively[1]. BMS 299897 is a selective inhibitor for gamma-secretase. Reductions in the formation of Abeta peptides by gamma-secretase inhibitors may be a viable therapy for reducing Abeta in Alzheimer's disease. BMS-299897 is a gamma-secretase inhibitor that was effective in reducing amyloid beta-peptide (A beta) in transgenic mice and guinea pigs[3]. in vitro: BMS-299897 dose-dependently increased brain concentrations of APP carboxy-terminal fragments, consistent with inhibition of gamma-secretase. BMS-299897 (100 mg/kg po) reduced brain and plasma Abeta(1-40) rapidly (within 20min) and maximally within 3 h. BMS-299897 dose-dependently reduced cortical, cerebrospinal fluid (CSF), and plasma Abeta in guinea pigs with ED(50) values of 30 mg/kg intraperitoneally, without affecting CSF levels of alpha-sAPP. The reductions in cortical Abeta correlated significantly with the reductions in both plasma (r(2) = 0.77) and CSF (r(2) = 0.61) Abeta [1]. in vivo: BMS-299897blocked the Aβ(25-35)-induced deficits in spontaneous alternation or novel object recognition, using a 1h intertrial time interval. BMS-299896 failed to affect the passive avoidance impairments or novel object recognition, using a 24h intertrial time interval [2]. Clinical trial: Study to Evaluate the Safety, Pharmacokinetics and Tolerability of BMS-299897 .Phage I.you can refer to more information at http://www.medchemexpress.com
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