Rapamycin (Synonyms:雷帕霉素; 西罗莫司; Sirolimus; AY-22989)
目录号 : KM2292 CAS No. : 53123-88-9

Rapamycin (Sirolimus) 是一种有效且特异性的 mTOR 抑制剂,作用于 HEK293 细胞,抑制 mTOR,IC50 为 0.1 nM。Rapamycin 与 FKBP12 结合且抑制 mTORC1。Rapamycin 还是一种自噬 (autophagy) 激活剂,免疫抑制剂。

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Other Forms of Rapamycin:

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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.

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.

Cell Viability Assay

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.

Western Blot Analysis

Cell Line: 95D cells
Concentration: 10 nM and 20 nM
Incubation Time: 24 hours
Result: Combination treatment with RP-56976 decreased phosphorylation of ERK.
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.

Animal Model: 24 male nu/nu mice aged 4-5 week old (15-20 g)
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.
分子式
C51H79NO13
分子量
914.17
CAS号
53123-88-9
中文名称
雷帕霉素;西罗莫司
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
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (136.74 mM; Need ultrasonic)

Ethanol : 50 mg/mL (54.69 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.0939 mL 5.4694 mL 10.9389 mL
5 mM 0.2188 mL 1.0939 mL 2.1878 mL
10 mM 0.1094 mL 0.5469 mL 1.0939 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% EtOH    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (2.73 mM); Suspended solution

    此方案可获得 ≥ 2.5 mg/mL (2.73 mM,饱和度未知) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% EtOH    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (2.73 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (2.73 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% EtOH    90% corn oil

    Solubility: ≥ 2.5 mg/mL (2.73 mM); Suspended solution

    此方案可获得 ≥ 2.5 mg/mL (2.73 mM,饱和度未知) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 900 μL玉米油中,混合均匀。

  • 4.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (2.28 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.28 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 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 5.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (2.28 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (2.28 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 6.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (2.28 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.28 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    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 μL玉米油中,混合均匀。

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The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
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