Chemical Structure : DDR1-IN-2
CAS No.:
1315329-35-1
DDR1-IN-2
Catalog No.: PC-24448Not For Human Use, Lab Use Only.
DDR1-IN-2 is a potent and selective inhibitor of DDR1 receptor tyrosine kinase with IC50 of 47.6 nM, 4-fold selective over DDR-2 (IC50=145 nM), inhibits DDR1 autophosphorylation in cells.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
DDR1-IN-2 is a potent and selective inhibitor of DDR1 receptor tyrosine kinase with IC50 of 47.6 nM, 4-fold selective over DDR-2 (IC50=145 nM), inhibits DDR1 autophosphorylation in cells.
DDR1-IN-2 exhibits excellent selectivity for DDR1 with selectivity score (S(1) at 1 μM) of 0.07 as assessed using the KinomeScan approach.
DDR1-IN-2 blocks collagen induced DDR1 autophosphorylation in U2OS cells with EC50 of 9.45 nM.
DDR1-IN-2 exhibits anti-proliferation effect against a panel of different cancer cell lines (HCT-116(OWT), IC50=0.81 uM).
Physicochemical Properties
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M.Wt
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580.66
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Formula
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C31H35F3N6O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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4-((4-ethylpiperazin-1-yl)methyl)-N-(3-(((4-methoxy-1H-pyrrolo[2,3-b]pyridin-5-yl)methyl)amino)-4-methylphenyl)-3-(trifluoromethyl)benzamide
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References
1. Kim HG, et al.ACS Chem Biol. 2013 Oct 18;8(10):2145-50.
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