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| CAS号 | 53123-88-9 | 产地 | 进口 |
|---|---|---|---|
| 级别 | 其他 | 证书 | ISO系列证书 |
注：本产品仅用于科研，不可用于临床
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
体外研究
(In Vitro)
Rapamycin（12.5-100 nM；24 小时）处理在所有测试的细胞系（A549、SPC-A-1、95D 和 NCI-H446 细胞）中以剂量依赖性方式对肺癌细胞增殖产生适度抑制作用，达到约 100 nM 时细胞增殖减少 30-40%，而 12.5 nM 时减少约 10%[3]。
将肺癌细胞系 95D 细胞单独或联合暴露于 Rapamycin（10 nM、20 nM）和 RP-56976（1 nM、10 nM）（Rapamycin 20 nM + RP-56976 10 nM）。单独暴露于 Rapamycin 或 RP-56976 24 小时后，不会显着改变 ERK1/2 的表达或磷酸化水平，而 Rapamycin 与 RP-56976 联合处理的细胞表现出 ERK1/2 磷酸化水平的显着降低[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. |
体内研究
(In Vivo)
Rapamycin (2.0 mg/kg; 腹腔内注射; 每隔一天;28 天) 单独使用有中等的抑制作用。然而，与对照组、Rapamycin 组相比，metformin联合 Rapamycin 对肿瘤生长的抑制作用明显增强[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
性状
Solid
Formula
C51H79NO13
CAS 号
53123-88-9
中文名称
雷帕霉素；sirolimus
来源
bacterium Streptomyces hygroscopicus
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 months |
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