CP-673451|cas 343787-29-1| DC Chem|Supplier|Price|Buy  

CP-673451|cas 343787-29-1| DC Chem|Supplier|Price|Buy

DC Chemicals Supply: CP-673451, Cas: 343787-29-1 ,Cat No. DC7389, Purity>98%, In stock.

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CP-673451|cas 343787-29-1, Synonym name: CP 673451; CP673451, Chemical name:　1-(2-(5-(2-methoxyethoxy)-1H-benzo[d]imidazol-1-yl)quinolin-8-yl)piperidin-4-amine, Molecule weight: 417.5, Molecule Formula: C24H27N5O2

CP 673451 is a selective inhibitor of PDGFRα/β with IC50 of 10 nM/1 nM, exhibits >450-fold selectivity over other angiogenic receptors, has antiangiogenic and antitumor activity.

CP 673451 is a selective inhibitor of PDGFRα/β with IC50 of 10 nM/1 nM, exhibits >450-fold selectivity over other angiogenic receptors. 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. [2] CP 673451 (once-daily p.o. ?0 days dosing routinely) inhibits tumor growth (ED50 < 33 mg/kg) in a number of human tumor xenografts grown s.c. in athymic mice, including H460 human lung carcinoma, Colo205 and LS174T human colon carcinomas, and U87MG human glioblastoma multiforme. [1] In RUCH2 xenograft-bearing mice, CP 673451 reduces tumor growth and stromal cell infiltration. [2]