|(S)-4-(3-(丁-2-炔基)哌啶-1-基)-5-氟-2,3-二甲基-1H-吲哚-7-甲酰胺|CsnPharm

CAS No.: 1912445-55-6

(S)-4-(3-(but-2-ynamido)piperidin-1-yl)-5-fluoro-2,3-dimethyl-1H-indole-7-carboxamide Catalog No. CSN24257

Synonyms: BMS-986195;branebrutinib

BMS-986195 is a potent, covalent, irreversible BTK inhibitor with IC50 value of 0.1nM.

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生物活性

实验方案

技术信息

生物活性

描述Bruton's tyrosine kinase (BTK), a non-receptor tyrosine kinase, is a member of the Tec family of kinases and is essential for B cell receptor (BCR) mediated signaling. BTK also plays a critical role in the downstream signaling pathways for the Fcγ receptor in monocytes, the Fcε receptor in granulocytes, and the RANK receptor in osteoclasts ^[1]. BMS-986195 is a highly potent, selective covalent, irreversible inhibitor of BTK with an IC₅₀ value of 0.1 nM ^[1]. BMS-986195 was highly effective at inhibiting TNFα production with equivalent potency to those measured for the BCR-dependent end points in B cells. In human whole blood assays, it potently inhibited BCR-stimulated expression of CD69 on B cells with an IC50 of 11 nM ^[1]. When administered orally to BALB/c mice, BMS-986195 dose-dependently inactivated BTK in peripheral blood with a single dose of 0.5 mg/kg, providing 90% inactivation 4 h after dosing. In addition, BMS-986195 provided a dose-dependent protection against pitting, loss of bone mass, woven porous bone, and fusion of the small bones evident in the mice receiving only vehicle ^[1].
作用机制The tetrahydrocarbazole NH and the carboxamide carbonyl of BMS-986195 are engaged in a hydrogen bonding interaction with Met477 in the hinge region of the active site of BTK .
参考文献

[1] Watterson SH, Liu Q, Beaudoin Bertrand M, Batt DG, Li L, Pattoli MA, Skala S, Cheng L, Obermeier MT, Moore R, Yang Z, Vickery R, Elzinga PA, Discenza L, D'Arienzo C, Gillooly KM, Taylor TL, Pulicicchio C, Zhang Y, Heimrich E, McIntyre KW, Ruan Q, Westhouse RA, Catlett IM, Zheng N, Chaudhry C, Dai J, Galella MA, Tebben AJ, Pokross M, Li J, Zhao R, Smith D, Rampulla R, Allentoff A, Wallace MA, Mathur A, Salter-Cid L, Macor JE, Carter PH, Fura A, Burke JR, Tino JA. Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK). J Med Chem. 2019 Apr 11;62(7):3228-3250. doi: 10.1021/acs.jmedchem.9b00167. Epub 2019 Mar 29. PMID: 30893553.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6996 mL
- 13.4982 mL
- 26.9963 mL
- 5 mM
- 0.5399 mL
- 2.6996 mL
- 5.3993 mL
- 10 mM
- 0.2700 mL
- 1.3498 mL
- 2.6996 mL

技术信息

CAS号

1912445-55-6

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H23FN4O2

运输

蓝冰

分子量

370.42

别名

BMS-986195;branebrutinib

溶解度

DMSO	125.0 mg/mL (337.5 mM)
Water	insoluble

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(S)-4-(3-(but-2-ynamido)piperidin-1-yl)-5-fluoro-2,3-dimethyl-1H-indole-7-carboxamide Catalog No. CSN24257

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