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Products are for research use only. Not for human use. We do not sell to patients.
(CP 673451; CP673451)
CP-673451 Chemical Structure
|Product name: CP-673451|
|Cat. No.: HY-12050|
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.
IC50 value: 10 nM/1 nM(PDGFRα/β) 
in vitro: 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) . 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 .
in vivo: 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 . In RUCH2 xenograft-bearing mice, CP 673451 reduces tumor growth and stromal cell infiltration .
|M.Wt||417.5||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
100 mM in DMSO; Water < 1 mg/ml
|1 mg||5 mg||10 mg|
|1 mM||2.3952 mL||11.9760 mL||23.9521 mL|
|5 mM||0.4790 mL||2.3952 mL||4.7904 mL|
|10 mM||0.2395 mL||1.1976 mL||2.3952 mL|
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