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DDR1-IN-2

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

M.Wt 580.66
Formula C31H35F3N6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

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

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