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CAS No. : 1271022-90-2
MCE 国际站:BMS-911543
产品活性:BMS-911543 是一种选择性的 JAK2 抑制剂,IC50 值为 1.1 nM,对 JAK1,JAK3 和 TYK2 的选择性相对较弱,IC50 值分别为 75,360 和 66 nM。
研究领域:Epigenetics | Protein Tyrosine Kinase/RTK | JAK/STAT Signaling | Stem Cell/Wnt
作用靶点:JAK
In Vitro: BMS-911543 is a selective JAK2 inhibitor, with IC50s of 1.1 nM, less selective at JAK1, JAK3 and TYK2 (IC50, 75, 360, 66 nM, respectively). BMS-911543 displays IC50 of >25 μM for all targets except PDE4 (IC50, 5.6 μM). BMS-911543 exhibits potent antiproliferative effect on the SET-2 and BaF3-V617F engineered cell lines (both dependent upon JAK2 pathway), with IC50s of 60 and 70 nM, respectively, and such an effect on SET-2 and BaF3-V617F cells is correlated with similar activity on constitutively active pSTAT5 (IC50, 80 and 65 nM, respectively). BMS-911543 (>20 μM) is cytotoxic to murine or human pancreatic ductal adenocarcinoma (PDAC) cell lines. BMS-911543 (5 and 10 μM) also blocks T regulatory cell differentiation in vitro.
In Vivo: BMS-911543 is well tolerated up to 100 mg/kg in rats (mean AUC0-72 h, 11300 μM·h) and dogs (AUC0-24 h, 610 μM·h). A 15 mg/kg/day dose (Day 14 AUC0-24 h, 3200 μM·h) is well tolerated in two-week repeat dose studies in rats. BMS-911543 (30 mg/kg, p.o.) suppresses the growth of tumor and prolongs the median survival in KPC-Brca1 mice. BMS-911543 also selectively reduces pSTAT5 expression in pancreatic tumors and decreases levels of intratumoral FoxP3+ T regulatory cells in mice administered BMS-911543.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Epigenetics Compound Library | Immunology/Inflammation Compound Library | JAK/STAT Compound Library | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | Stem Cell Signaling Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Differentiation Inducing Compound Library | Reprogramming Compound Library | Chemical Probe Library | Anti-Breast Cancer Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Anti-Obesity Compound Library | Anti-Liver Cancer Compound Library | Anti-Prostate Cancer Compound Library | Cancer Stem Cells Compound Library | Pain-Related Compound Library | Highly Selective Inhibitors Library | JAK-IN-20 | JAK1-IN-9 | AT9283 | RO495 | TK4b | JAK-IN-17 | (E/Z)-Zotiraciclib | JAK-IN-10 | (3R,4S)-Tofacitinib | JAK3/BTK-IN-6 | Tyk2-IN-5 | Brevilin A | Broussonin E | Itacnosertib | RO8191 | Axltide | Fosifidancitinib | JAK3-IN-6 | Upadacitinib | JAK-IN-24 | AZD-1480 | Baricitinib-d3 | Tofacitinib-13C3 | AZ-3 | Delphinidin chloride | TK4g | Tofacitinib Prodrug-1
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