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首页-小分子抑制剂&激动剂-Tyrosine Kinase-BTK-BMS-986142
BMS-986142

Chemical Structure : BMS-986142

CAS No.: 1643368-58-4

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BMS-986142 (BMS 986142;BMS986142)

货号: PC-60422Not For Human Use, Lab Use Only.

BMS-986142 (BMS 986142) is a potent, selective and reversible BTK inhibitor with IC50 of 0.5 nM.

规格 价格 库存 数量
5 mg ￥2480 In stock
10 mg ￥3980 In stock
25 mg ￥5980 In stock
50 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BMS-986142 (BMS 986142) is a potent, selective and reversible BTK inhibitor with IC50 of 0.5 nM.
BMS-986142 displays 20-60-fold selectivity over Tec family kinases, >10,000-fold selectivity over JAK2.
BMS-986142 potently inhibits signaling and functional end points, including calcium flux (IC50=9 nM), production of cytokines, proliferation, and surface expression of CD86 (IC50=3-4 nM).
BMS-986142 potently inhibits BCR-stimulated expression of CD69 on B cells in human whole blood with IC50 of 90 nM.
BMS-986142 exhibits excellent in vivo properties and efficacy, and a very desirable tolerability and safety profile.

物理化学性质&存储条件

分子量 572.613
分子式 C32H30F2N4O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide

参考文献

1. Watterson SH, et al. J Med Chem. 2016 Oct 13;59(19):9173-9200.

2. Lee SK, et al. Eur J Clin Pharmacol. 2017 Jun;73(6):689-698.

3. Gillooly KM, et al. PLoS One. 2017 Jul 24;12(7):e0181782.

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