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CP-673451

CAS No. : 343787-29-1

MCE 站：CP-673451

产品活性：CP-673451 是一种有效的，选择性的血小板源生长因子受体 (PDGFR) 抑制剂，抑制 PDGFRα 和 PDGFRβ 的活性，IC₅₀ 值分别为 10 和 1 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：PDGFR

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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