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。
生物活性 | mTORinhibitor-8 is anmTORinhibitor andautophagyinducer.mTORinhibitor-8 inhibits the activity ofmTORvia FKBP12 and inducesautophagyof A549 human lungcancercells[1]. |
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体外研究 (In Vitro) | mTOR inhibitor-8 (Compound 5e; 0.1-10 μM; 24 and 48 hours) suppresses the growth of A549 cells in a dose-dependent manner[1]. 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[1]. 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[1]
Cell Viability Assay[1] 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 IC50of 2.6±0.11 μM. |
Western Blot Analysis[1] 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. |
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体内研究 (In Vivo) | mTOR inhibitor-8 (25 and 50 μM; 6 days) effectively inhibits tumor growth in vivo without adverse effect on normal chick chorioallantoic membrane angiogenesis[1].
Animal Model: | Fertile chicken eggs (7-9 days old)[1] | 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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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 | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 25 mg/mL(55.93 mM;Need ultrasonic) 配制储备液 1 mM | 2.2374 mL | 11.1869 mL | 22.3739 mL | 5 mM | 0.4475 mL | 2.2374 mL | 4.4748 mL | 10 mM | 0.2237 mL | 1.1187 mL | 2.2374 mL |
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此方案可获得 ≥ 2.08 mg/mL (4.65 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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