DDR1 inhibitor 7rh | DDR1 inhibitor | Probechem Biochemicals

Chemical Structure : DDR1 inhibitor 7rh

CAS No.: 1429617-90-2

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DDR1 inhibitor 7rh (DDR1-IN-7rh)

货号: PC-63518Not For Human Use, Lab Use Only.

DDR1 inhibitor 7rh is a potent, selective, ATP-competitive, orally available Discoidin domain receptor 1 (DDR1) inhibitor with IC50 of 6.8 nM in cell-free kinase assays.

规格	价格	库存
5 mg	￥980	In stock
10 mg	￥1480	In stock
25 mg	￥2680	In stock
50 mg	￥4580	In stock
100 mg		Get quote

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生物&药学活性

DDR1 inhibitor 7rh is a potent, selective, ATP-competitive, orally available Discoidin domain receptor 1 (DDR1) inhibitor with IC50 of 6.8 nM in cell-free kinase assays.
DDR1 inhibitor 7rh is significantly less potent in suppressing the kinase activities of DDR2 (IC50=101 nM), Bcr-Abl (IC50=355 nM), and c-Kit (IC50>10 uM).
DDR1 inhibitor 7rh inhibits DDR1-mediated signaling induced by soluble collagen (50 μg/ml) in a concentration-dependent manner, inhibits activation of PYK2 and PEAK1, signaling proteins downstream of DDR1 in PANC-1 cells.
DDR1 inhibitor 7rh induces significant decrease of total protein levels of DDR1 and Bcl-xL, causes a significant reduction in the level of MMP-2 in NSCLS cells.
DDR1 inhibitor 7rh suppresses the growth of K562 human CML cells with IC50 of 38 nM, A549, NCI-H23 and NCI-H460 human NSCLC cells with IC50 of 2.7, 2.1 and 3.0 µM, respectively.
DDR1 inhibitor 7rh abrogates collagen-induced DDR1 signaling in pancreatic tumor cells and consequently reduces colony formation and migration, exhibits striking efficacy in combination with chemotherapy in orthotopic xenografts and autochthonous pancreatic tumors.

物理化学性质&存储条件

分子量	546.598
分子式	C30H29F3N6O
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	4-Ethyl-N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)-3-(pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamide

参考文献

1. Aguilera KY, et al. Mol Cancer Ther. 2017 Nov;16(11):2473-2485.

2. Gao M, et al. J Med Chem. 2013 Apr 25;56(8):3281-95.

DDR1 inhibitor 7rh (DDR1-IN-7rh)

生物&药学活性

物理化学性质&存储条件

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DDR1 inhibitor 7rh (DDR1-IN-7rh)

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物理化学性质&存储条件

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