2125676-13-1
2125676-13-1 structure
- Name: DDR1 inhibitor 2.45
- Chemical Name: DDR1 inhibitor 2.45
- CAS Number: 2125676-13-1
- Molecular Formula: C23H20BrF3N6O3
- Molecular Weight: 565.351
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Discoidin Domain Receptor
- Create Date: 2020-01-20 16:42:55
- Modify Date: 2024-01-06 12:44:37
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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).
| Name | DDR1 inhibitor 2.45 |
|---|
| 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 |
|---|---|
| Molecular Weight | 565.351 |