DDR1-IN-1

Chemical Structure : DDR1-IN-1

CAS No.: 1449685-96-4

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货号: PC-24447Not For Human Use, Lab Use Only.

DDR1-IN-1 is a potent and selective inhibitor of DDR1 receptor tyrosine kinase with IC50 of 105 nM, 4-fold selective over DDR-2 (IC50=413 nM), inhibits DDR1 autophosphorylation in cells.

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5 mg	￥780	In stock
10 mg	￥1180	In stock
25 mg	￥2180	In stock
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生物&药学活性

DDR1-IN-1 is a potent and selective inhibitor of DDR1 receptor tyrosine kinase with IC50 of 105 nM, 4-fold selective over DDR-2 (IC50=413 nM), inhibits DDR1 autophosphorylation in cells.
DDR1-IN-1 exhibits excellent selectivity for DDR1 with a selectivity score (S(1) at 1 μM) of 0.01 as assessed using the KinomeScan approach.
DDR1-IN-1 blocks collagen induced DDR1 autophosphorylation in U2OS cells with EC50 of 86 nM.
DDR1-IN-1 binds to DDR1 in the 'DFG-out' conformation and inhibits DDR1 autophosphorylation in cells at submicromolar concentrations with good selectivity.
Inhibitors of PI3K and mTOR such as GSK2126458 potentiate the antiproliferative activity of DDR1-IN-1 in colorectal cancer cell lines.

物理化学性质&存储条件

分子量	552.60
分子式	C30H31F3N4O3
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-((4-Ethylpiperazin-1-yl)methyl)-N-(4-methyl-3-((2-oxoindolin-5-yl)oxy)phenyl)-3-(trifluoromethyl)benzamide

参考文献

1. Kim HG, et al.ACS Chem Biol. 2013 Oct 18;8(10):2145-50.

DDR1-IN-1

生物&药学活性

物理化学性质&存储条件

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