SB-505124 hydrochloride

CAS No.	356559-13-2	Cat. No.	BCP19172
Name	SB-505124 hydrochloride
Synonyms	SB 505124 hydrochloride;SB505124 hydrochloride;
Formula	C20H22ClN3O2	M. Wt	371.86

Description	in vitro: SB-505124 was identified as a potent inhibitor of the in vitro kinase activity of ALK5 for its substrate Smad3 with an IC50 of 47 ± 5 nM. This compound was determined to be a reversible ATP competitive inhibitor, because prior incubation of the ALK5 kinase with high concentrations of the inhibitor, followed by dilution to a sub-IC50concentration had no effect on the kinetics of Smad3 phosphorylation (data not shown). SB-505124 demonstrated no toxicity to renal epithelial A498 cells at concentrations up to 100 μM for 48 h. Selectivity of the SB-505124 inhibitor for type I receptors other than ALK5 was first evaluated against ALK4 and ALK2 in vitro. SB-505124 inhibited the closely related ALK4 with an IC50value of 129 ± 11 nM (about 2.5-fold less sensitive than ALK5) but did not inhibit ALK2 at concentrations up to 10 μM . The in vitro drug release study demonstrated 100% drug release within 12 h. The gel did not show cytotoxicity to the cultured rabbit subconjunctival cells by
Pathways	Angiogenesis/Protein Tyrosine Kinase TGF beta/Smad
Targets	BMP/TGF beta Receptor ALK

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