DDR inhibitor X

  Cat. No.:  DC10996   Featured
Chemical Structure
1644069-80-6
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Field of application
DDR inhibitor X is a potent discoidin domain receptor (DDR) inhibitor with IC50 of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM..
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)
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC11175 Dual DDR1 and DDR2 inhibitor 5n Dual DDR1 and DDR2 inhibitor 5n is a highly potent and selective small molecule inhibitor targeting both Discoidin Domain Receptor 1 (DDR1) and Discoidin Domain Receptor 2 (DDR2). These receptors are receptor tyrosine kinases (RTKs) that play critical roles in cell proliferation, migration, and extracellular matrix (ECM) remodeling. Dysregulation of DDR1 and DDR2 has been implicated in various diseases, including cancer, fibrosis, and inflammation, making them attractive therapeutic targets.
DC10996 DDR inhibitor X DDR inhibitor X is a potent discoidin domain receptor (DDR) inhibitor with IC50 of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM..
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