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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Discoidin Domain Receptor (DDR)-DDR1 inhibitor 2.45
DDR1 inhibitor 2.45

Chemical Structure : DDR1 inhibitor 2.45

CAS No.: 2125676-13-1

DDR1 inhibitor 2.45 (Compound 2.45)

货号: PC-35802Not For Human Use, Lab Use Only.

DDR1 inhibitor 2.45 (Compound 2.45) is a novel potent, selective, bioavailable Discoidin Domain Receptor 1 (DDR1) inhibitor with IC50 of 29 nM, displays 64-fold selectivity over DDR2 in biochemical assays.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

DDR1 inhibitor 2.45 (Compound 2.45) is a novel potent, selective, bioavailable Discoidin Domain Receptor 1 (DDR1) inhibitor with IC50 of 29 nM, displays 64-fold selectivity over DDR2 in biochemical assays.
DDR1 inhibitor 2.45 also possesses excellent kinome selectivity against a kinase panel of 468 kinases.
DDR1 inhibitor 2.45 inhibits DDR1 phosphorylation (70% inhibition at 1 uM in HT1080 cells overexpressing DDR1) and recruitment of SHC1 in vitro, and modulates phenotype of collagen stimulated renal epithelial cells.
DDR1 inhibitor 2.45 preserves renal function and reduces tissue damage in Col4a3−/− mice (the preclinical mouse model of Alport syndrome).

物理化学性质&存储条件

分子量 565.351
分子式 C23H20BrF3N6O3
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

2-(4-bromo-2-oxo-1'-(1H-pyrazolo[4,3-b]pyridine-5-carbonyl)spiro[indoline-3,4'-piperidin]-1-yl)-N-(2,2,2-trifluoroethyl)acetamide

参考文献

1. Richter H, et al. ACS Chem Biol. 2018 Nov 19. doi: 10.1021/acschembio.8b00866.

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