DDR inhibitor X

Cas No.:	1644069-80-6
Chemical Name:	N-[5-[[[(3-Fluorophenyl)carbamoyl]amino]methyl]-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide
SMILES:	C12=NC=C(C(NC3=CC(CNC(=O)NC4=CC=CC(F)=C4)=CC=C3C)=O)N1C=CC=C2
Formula:	C23H20FN5O2
M.Wt:	417.444
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[1]. Gordon Saxty, et al. Imidazo-condensed bicycles as inhibitors of discoidin domain receptors (ddrs)

Description:	DDR Inhibitor X is a potent discoidin domain receptor (DDR) inhibitor, with an IC50 of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM.
Target:	IC50: 3.3 nM (DDR2)[1] IC53: 1.5 nM (DDR1)[1]
In Vitro:	DDR Inhibitor (Example 6) is a potent DDR inhibitor, with an IC50 of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM[1].
Kinase Assay:	Europium Kinase binding assay is used. Compounds (DDR Inhibitor, etc.) are incubated with 0.5 nM DDR1 or 0.25 nM DDR2 for 1 hour at room temperature in low volume black 384 well assay plates containing 5 nM or 10 nM Kinase Tracer 178 respectively and 2 nM Europium labelled anti-GST antibody in assay buffer (50 mM HEPES pH 7.5, 10 mM MgCl2, 1 mM EGTA and 0.01 % BRIJ35). The ratio of fluorescence emission 665 nm/615 nm after excitation at 340 nm is obtained. IC50 values are determined from dose-response plots using nonlinear least-squares analysis[1].
References:	[1]. Gordon Saxty, et al. Imidazo-condensed bicycles as inhibitors of discoidin domain receptors (ddrs)