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DDR1 inhibitor 2.45

Chemical Structure : DDR1 inhibitor 2.45

CAS No.: 2125676-13-1

DDR1 inhibitor 2.45 (Compound 2.45)

Catalog No.: PC-35802Not For Human Use, Lab Use Only.

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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.
DDR1 inhibitor 2.45 also possesses excellent kinome selectivity against a kinase panel of 468 kinases.
DDR1 inhibitor 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.
DDR1 inhibitor 2.45 preserves renal function and reduces tissue damage in Col4a3−/− mice (the preclinical mouse model of Alport syndrome).

Physicochemical Properties

M.Wt 565.351
Formula C23H20BrF3N6O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(4-bromo-2-oxo-1'-(1H-pyrazolo[4,3-b]pyridine-5-carbonyl)spiro[indoline-3,4'-piperidin]-1-yl)-N-(2,2,2-trifluoroethyl)acetamide

References

1. Richter H, et al. ACS Chem Biol. 2018 Nov 19. doi: 10.1021/acschembio.8b00866.

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