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MedChemExpress (M

CAS	572924-54-0	純度	98.81%
分子量	990.21	分子式	C??H??NO??P
供貨周期	現(xiàn)貨	規(guī)格	5 mg
貨號	HY-50908	應(yīng)用領(lǐng)域	醫(yī)療衛(wèi)生,化工,生物產(chǎn)業(yè),制藥

Ridaforolimus (MK-8669) 是一種有效和選擇性的 mTOR 抑制劑，在 HT-1080 細(xì)胞中抑制 S6 磷酸化的 IC50 值為 0.2 nM。

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Ridaforolimus

CAS No. : 572924-54-0

MCE 國際站：Ridaforolimus

產(chǎn)品活性：Ridaforolimus (MK-8669) 是一種有效和選擇性的 mTOR 抑制劑，在 HT-1080 細(xì)胞中抑制 S6 磷酸化的 IC₅₀ 值為 0.2 nM。

研究領(lǐng)域：PI3K/Akt/mTOR | Autophagy | Anti-infection

作用靶點(diǎn)：mTOR | Autophagy | Bacterial

In Vitro: Treatment of HT-1080 fibrosarcoma cells with Ridaforolimus results in a dose-dependent inhibition of phosphorylation of both S6 and 4E-BP1, with IC₅₀s of 0.2 and 5.6 nM, respectively, and EC₅₀s of 0.2 and 1.0 nM, respectively. In HT-1080 cells, the EC₅₀ for inhibition of cell proliferation (0.5 nM) is similar to the EC₅₀s for inhibition of S6 and 4E-BP1 phosphorylation. Exposure to Ridaforolimus reduces the proliferation of cell lines representing a variety of tumor types. Administration of Ridaforolimus to tumor cells in vitro elicit dose-dependent inhibition of mTOR activity with concomitant effects on cell growth and division. Ridaforolimus exhibits a predominantly cytostatic mode of action, consistent with the findings for other mTOR inhibitors. Potent inhibitory effects on vascular endothelial growth factor secretion, endothelial cell growth, and glucose metabolism.

In Vivo: Ridaforolimus inhibits tumor growth in mice bearing PC-3 (prostate), HCT-116 (colon), MCF7 (breast), PANC-1 (pancreas), or A549 (lung) xenografts. Ridaforolimus inhibits tumor growth in a dose-dependent manner, with 0.3 mg/kg being the lowest dose that inhibits tumor growth significantly and 3 and 10 mg/kg doses achieving maximum inhibition.