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Signaling Pathway

CP-673451

HY-12050

(CP 673451; CP673451)

CP-673451

CP-673451 Chemical Structure

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.

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10 mM * 1 mL in DMSO $150 In-stock
5 mg $136 In-stock
10 mg $256 In-stock
50 mg $776 In-stock
100 mg $1050 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €147 In-stock
5 mg €133 In-stock
10 mg €251 In-stock
50 mg €760 In-stock
100 mg €1029 In-stock
200 mg Get quote
500 mg Get quote

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Product name: CP-673451
Cat. No.: HY-12050

CP-673451 Data Sheet

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    Purity: 99.58%

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Biological Activity of CP-673451

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) [1]
Target: 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) [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].
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 [1]. In RUCH2 xenograft-bearing mice, CP 673451 reduces tumor growth and stromal cell infiltration [2].

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 417.5 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C24H27N5O2
CAS No 343787-29-1
Solvent & Solubility

100 mM in DMSO; Water < 1 mg/ml

Preparing Stock Solutions

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

References on CP-673451

Inhibitor Kit

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