BMS-986202 | TYK2 inhibitor | Probechem Biochemicals

Chemical Structure : BMS-986202

CAS No.: 1771691-34-9

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BMS-986202 (BMS 986202)

货号: PC-38210Not For Human Use, Lab Use Only.

BMS-986202 (BMS 986202) is potent, selective Tyk2 inhibitor that binds to Tyk2 JH2 domain with IC50 of 0.19 nM, Ki of 0.02 nM, >10,000-fold over 273 kinases and pseudokinases.

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5 mg	￥2980	In stock
10 mg	￥4580	In stock
25 mg	￥7580	In stock
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100 mg		Get quote

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生物&药学活性

BMS-986202 (BMS 986202) is potent, selective Tyk2 inhibitor that binds to Tyk2 JH2 domain with IC50 of 0.19 nM, Ki of 0.02 nM, >10,000-fold over 273 kinases and pseudokinases.
BMS-986202 demonstrated cellular activity (IL-23 IC50=12 nM) in IL-23 stimulated reporter assay (in Kit225 T cells).
BMS-986202 also binds Jak1 JH2 with an IC50 of 7.8 nM, but this enzymatic binding did not lead to any functional activities, as BMS-986202 displayed an activity (IC50) of greater than 12.5 μM in the IL-2 stimulated Jak1/3-dependent cellular assay.
BMS-986202 showed in vivo efficacy in mouse models of IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus.

物理化学性质&存储条件

分子量	439.466
分子式	C22H18D3FN6O3
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-(Cyclopropanecarboxamido)-4-((3-(5-fluoropyrimidin-2-yl)-2-methoxyphenyl)amino)-N-(methyl-d3)nicotinamide

参考文献

1. Liu C, et al. J Med Chem. 2021 Jan 14;64(1):677-694.

BMS-986202 (BMS 986202)

生物&药学活性

物理化学性质&存储条件

参考文献

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BMS-986202 (BMS 986202)

生物&药学活性

物理化学性质&存储条件

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