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/ Rapamycin

西罗莫司 /Rapamycin 98%

货号：A656002 同义名： 雷帕霉素 / Sirolimus;AY-22989 Ambeed 开学季，买赠积分，赢豪礼

Rapamycin is a specific mTOR inhibitor with IC50 of ~0.1 nM.

Rapamycin 化学结构 CAS号：53123-88-9
Rapamycin 化学结构
CAS号：53123-88-9
Rapamycin 3D分子结构
CAS号：53123-88-9
Rapamycin 化学结构 CAS号：53123-88-9
Rapamycin 3D分子结构 CAS号：53123-88-9
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Rapamycin 纯度/质量文件 产品仅供科研

货号：A656002 标准纯度： 98%
批次查询： 批次纯度:

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产品名称 mTOR ↓ mTORC1 ↓ mTORC2 ↓ 其他靶点 纯度
AZD-8055 ++++

mTOR (full length), IC50: 0.8 nM

mTOR (truncated), IC50: 0.13 nM

 		99%+
Gedatolisib ++++

mTOR, IC50: 1.6 nM

 		98%
GSK1059615 ++

mTOR, IC50: 12 nM

 		98%
Vistusertib +++

mTOR, IC50: 2.8 nM

 		99%+
Torin 1 +++

mTOR, IC50: 4.32 nM

 		+++

mTORC1, IC50: 2 nM

 		++

mTORC2, IC50: 10 nM

 		DNA-PK 99%+
Dactolisib +++

mTOR (p70S6K), IC50: 6 nM

 		98+%
PI-103 +

mTOR, IC50: 30 nM

 		99%+
WAY-600 ++

mTOR, IC50: 9 nM

 		99%
Voxtalisib +

mTOR, IC50: 157 nM

 		99%+
PF-04691502 ++

mTOR, Ki: 16 nM

 		98+%
Onatasertib ++

mTOR, IC50: 16 nM

 		DNA-PK 99%+
Chrysophanol ✔ EGFR 98%
Samotolisib ✔ DNA-PK 99%+
Torkinib +++

mTOR, IC50: 8 nM

 		PDGFR,DNA-PK 99%+
Everolimus 99%+
WYE-354 +++

mTOR, IC50: 5 nM

 		98%
Tacrolimus ✔ 98%
PP121 ++

mTOR, IC50: 13 nM

 		PDGFR,VEGFR 99%+
Torin 2 ++++

mTOR, IC50: 0.25 nM

 		DNA-PK 99%+
Rapamycin ++++

mTOR, IC50: ~0.1 nM

 		98%
GDC-0349 +++

mTOR, Ki: 3.8 nM

 		98%
XL388 ++

mTOR, IC50: 9.9 nM

 		+++

mTORC1, IC50: 8 nM

 		+

mTORC2, IC50: 166 nM

 		99%+
WYE-687 +++

mTOR, IC50: 7 nM

 		98+%
Apitolisib +

mTOR, Ki app: 17 nM

 		98%+
WYE-132 ++++

mTOR, IC50: 0.19 nM

 		99%+
Sapanisertib ++++

mTOR, Ki: 1.4 nM

 		99%+
BGT226 maleate ✔ 99%+
ETP-46464 ++++

mTOR, IC50: 0.6 nM

 		DNA-PK 98%
PI3K-IN-1 +

mTOR, IC50: 157 nM

 		98+%
Zotarolimus +++

FKBP-12, IC50: 2.8 nM

 		99+%
OSI-027 +++

mTOR, IC50: 4 nM

 		+

mTORC1, IC50: 22 nM

 		+

mTORC2, IC50: 65 nM

 		99%+
Ridaforolimus ++++

mTOR, IC50: 0.2 nM

 		99%+
Temsirolimus +

mTOR, IC50: 1.76 μM

 		99%
CZ415 ++

mTOR, pIC50: 8.07

 		99%+
SF2523 +

mTOR, IC50: 280 nM

 		DNA-PK 99%+
KU-0063794 ++

mTORC1, IC50: ~10 nM

 		++

mTORC2, IC50: ~10 nM

 		99%+
Omipalisib ++++

mTORC1, Ki: 0.18 nM

 		++++

mTORC2, Ki: 0.3 nM

 		99%+
Palomid 529 ✔ 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
产品名称 Autophagy ↓ 其他靶点 纯度
SBI-0206965 +++

ULK2, IC50: 711 nM

ULK1, IC50: 108 nM

 		97%
Hydroxychloroquine sulfate ✔ 99%
Valproic acid sodium ✔ HDAC 97%
PFK-015 ++

PFKFB3, IC50: 207 nM

 		99%+
MRT68921 hydrochloride ++++

ULK2, IC50: 1.1 nM

ULK1, IC50: 2.9 nM

 		99%+
ROC-325 ✔ 99%+
Autophinib +++

Autophagy, IC50: 40 nM

 		97%
Lys05 ✔ 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Rapamycin 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.

Rapamycin 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
A253 Growth Inhibition Assay IC50=4.02101 μM SANGER

Rapamycin 动物研究

Dose Rat: 1 mg/kg , 3 mg/kg[1] (i.p.), 40 mg/kg[2] (i.p.)
Mice: 0.03 mg/kg - 0.7 mg/kg[3] (i.n.); 0.08 mg/kg[3] (i.p.), 40 mg/kg[4] (i.p.)
Administration i.p., i.n.

Rapamycin 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.

Rapamycin 实验方案

计算器
存储液制备 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

Rapamycin 技术信息

CAS号53123-88-9
分子式C51H79NO13
分子量 914.17
别名 雷帕霉素 ;Sirolimus;AY-22989;D00753;C07909;SILA 9268A;SLM;RPM;RAP;RAPA;Wy 090217;NSC 226080;NSC-2260804;Rapamune
运输蓝冰
存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -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

Tags: Rapamycin | Sirolimus;AY-22989;D00753;C07909;SILA 9268A;SLM;RPM;RAP;RAPA;Wy 090217;NSC 226080;NSC-2260804;Rapamune | 雷帕霉素 | Autophagy | mTOR | AmBeed-信号通路专用抑制剂 | Rapamycin 纯度/质量文件 | Rapamycin 亚型比较 | Rapamycin 生物活性 | Rapamycin 细胞研究 | Rapamycin 动物研究 | Rapamycin 参考文献 | Rapamycin 实验方案 | Rapamycin 技术信息

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