DDR1 inhibitor 2.45 structure
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Common Name | DDR1 inhibitor 2.45 | ||
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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 2.45DDR1 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). |
Name | DDR1 inhibitor 2.45 |
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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). |
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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) |
Molecular Formula | C23H20BrF3N6O3 |
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Molecular Weight | 565.351 |