CP-673451

Research use only, not for human use.

CP-673451 is a selective inhibitor of PDGFRα/β with IC50 of 10 nM/1 nM.

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.(In Vitro):CP-673451 efficiently suppresses the PDGFR downstream signaling pathway. It inhibits phosphorylation of Akt, GSK-3β, p70S6, and S6 in A549 cells in a concentration-dependent manner. CP-673451 (0.0625-4 μM) significantly reduces the viability of NSCLC cell lines A549 and H1299 in a time- and concentration-dependent manner, with IC50s of 0.49 and 0.61 μM, respectively. CP-673451 (1, 4 μM) induces apoptosis in non-small-cell lung cancer cells. CP-673451 (25, 100, or 400 nM) is effective at inhibiting migration and invasion of NSCLC cells by suppression of lamellipodia formation. CP-673451 and crenolanib show selective lethality toward cells with CA. U2OS cells treated with 1 to 4 μM CP-673451 or crenolanib show a ruffled cell surface as a sign for alterations of the cortical actin cytoskeleton. CP-673451 attenuates PDGF-BB-induced signaling, and significantly enhances the phosphorylation of PDGFR-β downstream effectors, Akt and MEK. CP-673,451 (0.5 μM) regulates cell proliferation through mechanisms involving reduced phosphorylation of GSK-3α and GSK-3β. CP-673,451 impairs rhabdosphere-forming capacity in both RD and RUCH2 cultures. CP-673,451 inhibits PDGFR-β in PAE-β cells with an IC50 value of 6.4 nM. Besides, CP-673,451 incubation in H526 and PAE-β cells results in an IC50 value of 1.1 μM against c-kit.(In Vivo):CP-673451 (20 mg/kg) leads to a medium suppression of tumor growth, while high-dose CP-673451 (40 mg/kg) strongly inhibits tumor growth in mice without significant weitht loss. CP-673,451 (10, 33, and 100 mg/kg, p.o., b.i.d) inhibits the growth of Colo205 tumor in a dose-dependent manner, and similar tumor growth inhibition experiments completes on LS174T, H460, and U87MG xenografts, with no signs of morbidity or weight loss.

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CP-673451 | CP673451 | CP 673451 | CP-673,451

Angiogenesis

c-Kit

c-Kit| PDGFRα| PDGFRβ| VEGFR1| VEGFR2

Cancer

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343787-29-1

417.5

C24H27N5O2

>98% (HPLC)

DMSO:28 mg/mL warmed (67.06 mM); Ethanol:4 mg/mL (9.58 mM); Water:<1 mg/mL (<1 mM)

NC1CCN(C2=C3N=C(N4C5=CC=C(OCCOC)C=C5N=C4)C=CC3=CC=C2)CC1

1-(2-(5-(2-Methoxyethoxy)benzimidazol-1-yl)quinolin-8-yl)piperidin-4-ylamine

(-20℃)

With Ice Pack

≥ 2 years