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产品介绍
产品信息
商品描述
BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor(IC50 = 1.6 nM).
分子量
382.07
纯度
98%
可溶性
DMSO:25 mg/mL (65.31 mM)
In vitro(体外研究)
BMS-986260 demonstrated functional activity in multiple TGFβ-dependent cellular assays, excellent kinome selectivity, favorable pharmacokinetic properties, and curative in vivo efficacy in combination with anti-PD-1 antibody in murine colorectal cancer (CRC) models. Since daily dosing of TGFβR1 inhibitors is known to cause class-based cardiovascular (CV) toxicities in preclinical species, a dosing holiday schedule in the anti-PD-1 combination efficacy studies was explored. An intermittent dosing regimen of 3 days on and 4 days off allowed mitigation of CV toxicities in one month dog and rat toxicology studies and also provided similar efficacy as once daily dosing.
背景
分子式
C18H12ClFN6O
CAS号
2001559-19-7
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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