注:本產品僅用于科研,不可用于臨床
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[1]. Rapamycin is an autophagy activator, an immunosuppressant
體外研究
(In Vitro)
Rapamycin(12.5-100 nM;24 小時)處理在所有測試的細胞系(A549、SPC-A-1、95D 和 NCI-H446 細胞)中以劑量依賴性方式對肺癌細胞增殖產生適度抑制作用,達到約 100 nM 時細胞增殖減少 30-40%,而 12.5 nM 時減少約 10%[3]。
將肺癌細胞系 95D 細胞單獨或聯合暴露于 Rapamycin(10 nM、20 nM)和 RP-56976(1 nM、10 nM)(Rapamycin 20 nM + RP-56976 10 nM)。單獨暴露于 Rapamycin 或 RP-56976 24 小時后,不會顯著改變 ERK1/2 的表達或磷酸化水平,而 Rapamycin 與 RP-56976 聯合處理的細胞表現出 ERK1/2 磷酸化水平的顯著降低[3]。
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[3]
Cell Line: | Lung cancer cell lines A549, SPC-A-1, 95D and NCI-H446 |
Concentration: | 12.5 nM, 25 nM, 50 nM, 100 nM |
Incubation Time: | 24 hours |
Result: | Treatment exerted modest inhibitory effect on lung cancer cell proliferation in a dose-dependent manner in all cell lines. |
體內研究
(In Vivo)
Rapamycin (2.0 mg/kg; 腹腔內注射; 每隔一天;28 天) 單獨使用有中等的抑制作用。然而,與對照組、Rapamycin 組相比,metformin聯合 Rapamycin 對腫瘤生長的抑制作用明顯增強[4]。
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: | 24 male nu/nu mice aged 4-5 week old (15-20 g)[4] |
Dosage: | 2.0 mg/kg |
Administration: | Intraperitoneal injection; every other day; 28 days |
Result: | Had a moderate inhibitory effect in monotherapy group. The combination with Metformin exerted a significantly increased inhibition of tumor growth. |
Clinical Trial
NCT Number | Sponsor | Condition | Start Date | Phase |
---|---|---|---|---|
NCT03826628 | Dermatology Specialties Limited Partnership | July 28, 2019 | Phase 2|Phase 3 | |
NCT05556681 | C. R. Bard | August 2, 2022 | ||
NCT01223755 | Mario Negri Institute for Pharmacological Research |
分子量
914.17
性狀
Solid
Formula
C51H79NO13
CAS 號
53123-88-9
中文名稱
雷帕霉素;sirolimus
來源
bacterium Streptomyces hygroscopicus
運輸條件
Room temperature in continental US; may vary elsewhere.
儲存方式
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 months |