CP-673451|343787-29-1|-陌孚医药/Medlife

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CP-673451

目录号: PL08998 纯度: ≥99%

CAS No. :343787-29-1

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中文名称	CP-673451
中文别名	1-[2-[5-(2-甲氧基乙氧基)苯并咪唑-1-基]喹啉-8-基]哌啶-4-基胺;1-{2-[5-(2-甲氧基-乙氧基)-苯并咪唑-1-基]-喹啉-8-基}-哌啶-4-胺;CP673451 抑制剂;CP-673451 抑制剂
英文名称	CP-673451
英文别名	CP 673451;4-Piperidinamine,1-[2-[5-(2-methoxyethoxy)-1H-benzimidazol-1-yl]-8-quinolinyl]-;CP-673451;1-[2-[5-(2-methoxyethoxy)benzimidazol-1-yl]quinolin-8-yl]piperidin-4-amine;1-{2-[5-(2-Methoxy-ethoxy)-benzoimidazol-1-yl]-quinolin-8-yl}-piperidin-4-ylamine;1-(2-(5-(2-methoxyethoxy)-1H-benzo[d]imidazol-1-yl)quinolin-8-yl)piperidin-4-amine;1-[2-[5-(2-Methoxyethoxy)benzimidazol-1-yl]quinolin-8-yl]piperidin-4-ylamine;CS-0207;UNII-0AM0WWD90A;CP673451;0AM0WWD90A;1-(2-(5-(2-Methoxyethoxy)benzimidazol-1-yl)quinolin-8-yl)piperidin-4-ylamine;1-{2-[5-(2-Methoxy
Cas No.	343787-29-1
分子式	C₂₄H₂₇N₅O₂
分子量	417.50
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	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。
生物活性	CP-673451 is a potent and selective inhibitor of PDGFR with IC 50 s of 10 and 1 nM for PDGFRα and PDGFRβ, respectively.
性状	Solid
IC50 & Target[1][2]	PDGFRα 10 nM (IC50) PDGFRβ 1 nM (IC50
体外研究(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
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Xi Y, et al. CP-673451, a platelet-derived growth-factor receptor inhibitor, suppresses lung cancer cell proliferation and migration. Onco Targets Ther. 2014 Jul 3;7:1215-21. [2]. Konotop G, et al. Pharmacological Inhibition of Centrosome Clustering by Slingshot-Mediated Cofilin Activation and Actin Cortex Destabilization. Cancer Res. 2016 Nov 15;76(22):6690-6700

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (239.52 mM)配制储备液

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2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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