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) |