mTOR inhibitor-8

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

mTOR inhibitor-8 是一种 mTOR 抑制剂和自噬 (autophagy) 诱导剂。mTOR inhibitor-8 通过 FKBP12 抑制 mTOR 活性，并诱导 A549 人肺癌细胞自噬。

mTOR inhibitor-8 is an mTOR inhibitor and autophagy inducer.mTOR inhibitor-8 inhibits the activity of mTOR via FKBP12 and induces autophagy of A549 human lung cancer cells.

mTOR inhibitor-8 (Compound 5e; 0.1-10?μM; 24 and 48 hours) suppresses the growth of A549 cells in a dose-dependent manner.mTOR inhibitor-8 induces autophagy in an mTOR-dependent manner. mTOR inhibitor-8 (10?μM; 3-24?hours) induces autophagy in a time-dependent manner. The levels of LC3B-II are enhanced.mTOR inhibitor-8 (10?μM; 3-24?hours)reduces the phosphorylation of RPS6KB1 (ribosomal protein S6 kinase) and EIF4EBP1 (eukaryotic translation initiation factor 4E-binding protein 1), two essential substrates of mTOR Cell Viability Assay Cell Line:A549 cells Concentration:0.1, 1, 5, 10?μM Incubation Time:24 and 48 hours Result:Suppressed the growth of A549 cells with an IC50 of 2.6±0.11 μM.Western Blot Analysis Cell Line:A549 cells Concentration:10?μM Incubation Time:3, 6, 12 and 24?hours Result:The levels of phosphorylation of RPS6KB1 and EIF4EBP1 were significantly decreased after treatment.

mTOR inhibitor-8 (25 and 50 μM; 6 days) effectively inhibits tumor growth in vivo without adverse effect on normal chick chorioallantoic membrane angiogenesis.Animal Model:Fertile chicken eggs (7-9 days old) Dosage:25 and 50 μM Administration:6 days Result:Significant xenograft tumor remission was observed in eggs compared with the DMSO-treated eggs.

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PI3K/Akt/mTOR signaling

mTOR

mTOR | Autophagy

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2489196-70-3

446.95

C24H19ClN4OS

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 25 mg/mL (55.93 mM; 超声助溶 )

COc1ccc(cc1)C1CC(=NN1c1nc(cs1)-c1ccncc1)c1ccc(Cl)cc1

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(-20℃)

With Ice Pack

≥ 2 years