Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BMS-911543 是一种选择性 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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 469 | 现货 | ||
2 mg | ¥ 688 | 现货 | ||
5 mg | ¥ 957 | 现货 | ||
10 mg | ¥ 1,750 | 现货 | ||
25 mg | ¥ 3,180 | 现货 | ||
50 mg | ¥ 4,590 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 987 | 现货 |
产品描述 | BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1 nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1/2. |
靶点活性 | TYK2:75nM, AK1:1.1 nM, JAK3:350nM |
体外活性 | BMS-911543 shows potent antiproliferative activity in the SET-2 as well as BaF3-V617F engineered cell lines (both dependent upon JAK2 pathway), with IC50 values of 60 and 70 nM, respectively. The antiproliferative activity of BMS-911543 in SET-2 and BaF3-V617F cells correlates with similar activity on constitutively active pSTAT5 (IC50 80 and 65 nM, respectively). In contrast, non-JAK2-dependent cell lines (A549, MDA-MB-231, MiaPaCa-2) are significantly less sensitive to the inhibitor treatment. The excellent biochemical selectivity versus JAK1/3 translates to good cellular and functional selectivity in an IL-2 mediated T-cell proliferation assay (IC50 990 nM). Also, cell lines that rely on other JAK family members, including CTLL2 and parental BaF3 cells stimulated with IL-3, shows weak antiproliferative activity for BMS-911543 (IC50 2.9 and 3.5 μM, respectively)[1]. |
体内活性 | BMS-911543 suppresses the pSTAT5 levels (mediated by wild type JAK2) relative to vehicle control when stimulated with thrombopoetin (TPO) in a mouse pharmacodynamic model. The responses are dose dependent and results in nearly complete normalization of pSTAT5 levels for 18 h at the highest oral dose of 30 mg/kg. At an intermediate 10 mg/kg oral dose, ~65% reduction is observed up to 18 h, whereas at the 5 mg/kg dose, approximately 50% reduction in pSTAT5 for 8 h is achieved. Observed pSTAT5 reductions correlates with exposures of BMS-911543, with AUC0–8h values of 23, 41, and 109 μM·h, respectively, for dose levels of 5, 10, and 30 mg/kg. In addition, BMS-911543 demonstrates a potent and sustained (2 mg/kg up to 7 h) PD effect in blocking pSTAT5 formation in mice grafted with human SET-2 cells harboring JAK2-V617F mutation. The absolute oral bioavailability in solution is >50% in mice, rats, dogs, and monkeys. In addition, the absorption of BMS-911543 is not significantly impacted by particle dissolution (suspension formulation), with a relative bioavailability (vs solution) of ~60% in rats and ~100% in dogs[1]. |
别名 | BMS911543 |
分子量 | 432.52 |
分子式 | C23H28N8O |
CAS No. | 1271022-90-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 34 mg/mL (78.6 mM)
Ethanol: 21 mg/mL (48.6 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.312 mL | 11.5602 mL | 23.1203 mL | 57.8008 mL |
5 mM | 0.4624 mL | 2.312 mL | 4.6241 mL | 11.5602 mL | |
10 mM | 0.2312 mL | 1.156 mL | 2.312 mL | 5.7801 mL | |
20 mM | 0.1156 mL | 0.578 mL | 1.156 mL | 2.89 mL | |
DMSO | 50 mM | 0.0462 mL | 0.2312 mL | 0.4624 mL | 1.156 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
BMS-911543 1271022-90-2 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors Tyrosine Kinases JAK Histone Methyltransferase BMS 911543 Janus kinase inhibit Inhibitor BMS911543 inhibitor