Rapamycin

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Chemical Structure| 53123-88-9 同义名 : 雷帕霉素 ;Sirolimus;AY-22989;D00753;C07909;SILA 9268A;SLM;RPM;RAP;RAPA;Wy 090217;NSC 226080;NSC-2260804;Rapamune
CAS号 : 53123-88-9
货号 : A656002
分子式 : C51H79NO13
纯度 : 98%
分子量 : 914.17
MDL号 : MFCD00867594
存储条件：

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(131.27 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 50 mg/mL(54.69 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 4.6 mg/mL clear

PO 0.5% CMC-Na 45 mg/mL suspension

生物活性
靶点

  • mTOR

    mTOR, IC50:~0.1 nM
描述 Rapamycin inhibits endogenous mTOR activity in HEK293 cells with IC50 of ~0.1 nM, more potently than iRap and AP21967 with IC50 of ~5 nM and ~10 nM, respectively. In Saccharomyces cerevisiae, Rapamycin treatment induces a severe G1/S cell cycle arrest and inhibition of translation initiation to levels below 20% of control. Rapamycin significantly inhibits the cell viability of T98G and U87-MG in a dose-dependent manner with IC50 of 2 nM and 1 μM, respectively, while displaying little activity against U373-MG cells with IC50 of >25 μM despite the similar extent of the inhibition of mTOR signaling. Rapamycin (100 nM) induces G1 arrest and autophagy but not apoptosis in Rapamycin-sensitive U87-MG and T98G cells by inhibiting the function of mTOR.
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
697 Growth Inhibition Assay IC50=6.28 nM SANGER
8-MG-BA Growth Inhibition Assay IC50=581.52 nM SANGER
A101D Growth Inhibition Assay IC50=32.62 nM SANGER
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.09mL

0.22mL

0.11mL

5.47mL

1.09mL

0.55mL

10.94mL

2.19mL

1.09mL
参考文献

[1]Martin Hadamitzky and others, Repeated Systemic Treatment with Rapamycin Affects Behavior and Amygdala Protein Expression in Rats, International Journal of Neuropsychopharmacology, Volume 21, Issue 6, 1 June 2018, Pages 592–602, https://doi.org/10.1093/ijnp/pyy017

[2]Glover EM, Ressler KJ, Davis M. Differing effects of systemically administered rapamycin on consolidation and reconsolidation of context vs. cued fear memories. Learn Mem. 2010 Oct 29;17(11):577-81. doi: 10.1101/lm.1908310. PMID: 21036892; PMCID: PMC3256567.

[3]Yáñez JA, Forrest ML, Ohgami Y, Kwon GS, Davies NM. Pharmacometrics and delivery of novel nanoformulated PEG-b-poly(epsilon-caprolactone) micelles of rapamycin. Cancer Chemother Pharmacol. 2008 Jan;61(1):133-44. doi: 10.1007/s00280-007-0458-z. Epub 2007 Mar 29. PMID: 17393166; PMCID: PMC2259393.

[4]Blundell J, Kouser M, Powell CM. Systemic inhibition of mammalian target of rapamycin inhibits fear memory reconsolidation. Neurobiol Learn Mem. 2008 Jul;90(1):28-35. doi: 10.1016/j.nlm.2007.12.004. Epub 2008 Mar 7. PMID: 18316213; PMCID: PMC2497420.