BGB-8035 | BTK inhibitor | Probechem Biochemicals

Chemical Structure : BGB-8035

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BGB-8035 (BGB8035)

货号: PC-20324Not For Human Use, Lab Use Only.

BGB-8035 (BGB8035) is a potent, highly selective BTK inhibitor with IC50 of 1.1 nM, potently inhibits BTK Tyr223 phosphorylation in BTK pY223 cellular assays with IC50 of 13.9 nM.

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生物&药学活性

BGB-8035 (BGB8035) is a potent, highly selective BTK inhibitor with IC50 of 1.1 nM, potently inhibits BTK Tyr223 phosphorylation in BTK pY223 cellular assays with IC50 of 13.9 nM.
BGB-8035 shows IC50 of 10.4 nM in Rec-1-cell viability assays.
BGB-8035 is quite clean in the Cerep panel, and against a panel of 369 human kinases was evaluated displays < 70% inhibition against 359 kinases and>70% inhibition against 10 kinases, including BTK, a panel of 369 human kinases at 2 uM.
BGB-8035 (7.5 mg/kg BID) showed similar activity as ibrutinib at 50 mg/kg QD in the REC-1 xenograft model, showed tuomor growth inhibition.
BGB-8035 (10 mg/kg BID, oral) prevented the CIA model-associated body weight, induced dose-dependent inhibition of paw swelling in the collagen antibody-induced arthritis (CAIA) mouse model.

物理化学性质&存储条件

分子量	453.54
分子式	C24H31N5O4
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	(S)-7-(1-acryloylpiperidin-4-yl)-2-(3,5-dimethoxy-4-methylphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide

参考文献

1. Yunhang Guo, et al. J Med Chem. 2023 Mar 23;66(6):4025-4044.

BGB-8035 (BGB8035)

生物&药学活性

物理化学性质&存储条件

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BGB-8035 (BGB8035)

生物&药学活性

物理化学性质&存储条件

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