CP-673451
CAS No. | 343787-29-1 | Cat. No. | BCP04764 |
Name | CP-673451 | ||
Synonyms | CP673451;CP 673451; | ||
Formula | C24H27N5O2 | M. Wt | 417.5 |
Description | In glioblastoma tumors, CP-673451 (33 mg/kg) provides >50% inhibition of PDGFR-β receptor for 4 hours corresponding to an EC50 of 120 ng/mL in plasma at Cmax. In a sponge angiogenesis model, CP-673451 inhibits 70% of PDGF-BB-stimulated angiogenesis at a dose of 3 mg/kg (q.d. ×5, p.o., corresponding to 5.5 ng/mL at Cmax).[1] CP-673451 decreases cell proliferation rate through mechanisms involving reduced phosphorylation of GSK-3α and GSK-3β. In both RD and RUCH2 cultures, CP-673451 impairs rhabdosphere-forming capacity and cell differentiation, causes increased senescence. | ||
Pathways | Angiogenesis/Protein Tyrosine Kinase | ||
Targets | PDGFR |
Structure
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