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BMS986260
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BMS986260图片
CAS NO:2001559-19-7
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议

产品介绍
BMS986260是一种口服有活力的选择性TGFβR1抑制剂,是免疫肿瘤学药物。它能够抑制 MINK 和 NHLF 细胞系中 TGFβ 介导的 pSMAD2/3 核转位,IC50值分别为 350 nM 和 190 nM。它对 TGFβR1 的选择比 TGFβR2 同功酶高。

产品描述

BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor(IC50 = 1.6 nM).

体外活性

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.

Cas No.

2001559-19-7

分子式

C18H12ClFN6O

分子量

382.78

储存和溶解度

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years