DDR1 inhibitor 2.45

Modify Date: 2024-01-06 12:44:37

DDR1 inhibitor 2.45 Structure
DDR1 inhibitor 2.45 structure
Common Name DDR1 inhibitor 2.45
CAS Number 2125676-13-1 Molecular Weight 565.351
Density N/A Boiling Point N/A
Molecular Formula C23H20BrF3N6O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of DDR1 inhibitor 2.45


DDR1 inhibitor 2.45 (Compound 2.45) is a novel potent, selective, bioavailable Discoidin Domain Receptor 1 (DDR1) inhibitor with IC50 of 29 nM, displays 64-fold selectivity over DDR2 in biochemical assays; also possesses excellent kinome selectivity against a kinase panel of 468 kinases; Compound 2.45 inhibits DDR1 phosphorylation (70% inhibition at 1 uM in HT1080 cells overexpressing DDR1) and recruitment of SHC1 in vitro, and modulates phenotype of collagen stimulated renal epithelial cells; Compound 2.45 preserves renal function and reduces tissue damage in Col4a3−/− mice (the preclinical mouse model of Alport syndrome).

 Names

Name DDR1 inhibitor 2.45

 DDR1 inhibitor 2.45 Biological Activity

Description DDR1 inhibitor 2.45 (Compound 2.45) is a novel potent, selective, bioavailable Discoidin Domain Receptor 1 (DDR1) inhibitor with IC50 of 29 nM, displays 64-fold selectivity over DDR2 in biochemical assays; also possesses excellent kinome selectivity against a kinase panel of 468 kinases; Compound 2.45 inhibits DDR1 phosphorylation (70% inhibition at 1 uM in HT1080 cells overexpressing DDR1) and recruitment of SHC1 in vitro, and modulates phenotype of collagen stimulated renal epithelial cells; Compound 2.45 preserves renal function and reduces tissue damage in Col4a3−/− mice (the preclinical mouse model of Alport syndrome).
References References 1. Richter H, et al. ACS Chem Biol. 2018 Nov 19. doi: 10.1021/acschembio.8b00866. View Related Products by Target Discoidin Domain Receptor (DDR)

 Chemical & Physical Properties

Molecular Formula C23H20BrF3N6O3
Molecular Weight 565.351
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