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Rapamycin

CAS No. : 53123-88-9

MCE 國際站：Rapamycin

產品活性：Rapamycin (Sirolimus) 是一種有效且特異性的 mTOR 抑制劑，作用于 HEK293 細胞，抑制 mTOR，IC₅₀ 為 0.1 nM。Rapamycin 與 FKBP12 結合且抑制 mTORC1。Rapamycin 還是一種自噬 (autophagy) 激活劑，免疫抑制劑。

研究領域：PI3K/Akt/mTOR  |  Autophagy  |  Apoptosis  |  Immunology/Inflammation  |  Anti-infection  |  Metabolic Enzyme/Protease

作用靶點：mTOR  |  FKBP  |  Fungal  |  Autophagy  |  Endogenous Metabolite  |  Antibiotic  |  Bacterial

結構分類：抗生素  |  疾病研究  |  抗炎/免疫調劑  |  抗生素  |  大環內脂類  |  結構分類

In Vitro: 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.

In Vivo: 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.

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