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首页-小分子抑制剂&激动剂-TGF-beta/Smad-TGF beta Receptor (TGFBR)-BMS-986260
BMS-986260

Chemical Structure : BMS-986260

CAS No.: 2001559-19-7

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BMS-986260 (BMS986260)

货号: PC-72168Not For Human Use, Lab Use Only.

BMS-986260 (BMS 986260) is a potent, selective, and orally bioavailable TGFβR1 inhibitor with IC50 of 1.6 nM, negligible inhibition against TGFβR2 (IC50>15 uM).

规格 价格 库存 数量
5 mg ￥1580 In stock
10 mg ￥2380 In stock
25 mg ￥3980 In stock
50 mg ￥5980 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BMS-986260 (BMS 986260) is a potent, selective, and orally bioavailable TGFβR1 inhibitor with IC50 of 1.6 nM, negligible inhibition against TGFβR2 (IC50>15 uM).
BMS-986260 is a highly potent TGFβR1 inhibitor in both human (Kiapp=0.8 nM) and mouse (Kiapp=1.4 nM) biochemical assays, and displays exquisite selectivity for TGFβR1 over its isozyme TGFβR2, as well as in a panel of >200 kinases.
BMS-986260 inhibited phosphorylation and subsequent nuclear translocation of SMAD in mink lung epithelial (MvLu1) cells and normal human lung fibroblasts (NHLF) cells with IC50 of 0.35 and 0.19 uM, respectively, also inhibited TGFβ induced SMAD phosphorylation in NIH3T3 cell line, primary human T cells, and mouse and human whole blood, inhibited TGF-β mediated induction of Treg by downregulation of FOXP3 expression and a repression of CD25 with IC50 of 230 nM.
Combination of BMS-986260 with anti-PD-1-antibody demonstrated robust antitumor efficacy, correlated with pSMAD2/3 inhibition and increase in intratumoral CD8+ T-cells, BMS-986260 also inhibited metastasis to the lungs in a 4T1 syngeneic orthotopic mammary tumor model.

物理化学性质&存储条件

分子量 382.783
分子式 C18H12ClFN6O
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-(4-(3-Chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-1H-imidazol-5-yl)imidazo[1,2-b]pyridazine-3-carbonitrile

参考文献

1. Velaparthi U, et al. ACS Med Chem Lett. 2020 Jan 28;11(2):172-178.

2. Parrish KE, et al. Biopharm Drug Dispos. 2021 Apr;42(4):137-149.

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