Rapamycin是一种特异性mTOR 抑制剂，在 HEK293细胞中抑制mTOR时，IC50 为~0.1 nM。Rapamycin与 FKBP12 结合，并特异性地充当 mTORC1 的变构抑制剂。 Rapamycin是一种自噬激活剂和免疫抑制剂。
| CAS No. | 53123-88-9 |
| 生物活性 | Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant. |
| 分子式 | C51H79NO13 |
| 分子量 | 914.17 |
| 储存条件 | Powder -20℃ 3 years |
| 溶解性数据 | DMSO : 125 mg/mL (136.74 mM; Need ultrasonic) Ethanol : 50 mg/mL (54.69 mM; Need ultrasonic) |
| 体内研究 | Rapamycin (2.0 mg/kg; intraperitoneal injection; every other day; 28 days) alone has a moderate inhibitory effect. However, the combination of Metformin and Rapamycin exerts a significantly increased inhibition of tumor growth compared with the control group, the Rapamycin monotherapy group and the Metformin monotherapy group. |
| 体外研究 | Rapamycin (12.5-100 nM; 24 hours) treatment exerts modest inhibitory effect on lung cancer cell proliferation in a dose-dependent manner in all cell lines (A549, SPC-A-1, 95D and NCI-H446 cells) tested, achieving about 30-40% reduction in cell proliferation at 100 nM vs. ~10% reduction at 12.5 nM. Lung cancer cell line 95D cells are exposed to Rapamycin (10 nM, 20 nM) and RP-56976 (1 nM, 10 nM) alone or in combination (Rapamycin 20 nM+ RP-56976 10 nM). After 24 hours exposure to Rapamycin or RP-56976 alone does not significantly alter the level of expression or phosphorylation of ERK1/2, whereas cells treated with the combination of Rapamycin with RP-56976 exhibit a marked reduction in the phosphorylation levels of ERK1/2. |
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| 纯度及产品资料 | 98% |
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