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依维莫司 /Everolimus {[allProObj[0].p_purity_real_show]}

货号:A116645 同义名: RAD001;SDZ-RAD

Everolimus (RAD001)是雷帕霉素的衍生物,是一种强效、选择性、口服活性的 mTOR1 抑制剂。它与 FKBP-12 结合形成免疫抑制复合物,抑制肿瘤细胞增殖,诱导细胞凋亡自噬,表现出强效的免疫抑制和抗癌活性。

Everolimus 化学结构 CAS号:159351-69-6
Everolimus 化学结构
CAS号:159351-69-6
Everolimus 3D分子结构
CAS号:159351-69-6
Everolimus 化学结构 CAS号:159351-69-6
Everolimus 3D分子结构 CAS号:159351-69-6
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Everolimus 纯度/质量文件 产品仅供科研

货号:A116645 标准纯度: {[allProObj[0].p_purity_real_show]}
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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

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

mTOR, IC50: 5 nM

98%
Tacrolimus 98%
PP121 ++

mTOR, IC50: 13 nM

VEGFR,PDGFR 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

95%
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。

Everolimus 生物活性

靶点
  • mTOR

    mTOR (FKBP12), IC50:1.6 nM-2.4 nM

描述 Everolimus is an inhibitor of mTOR through binding FKBP12 with IC50 of 1.6-2.4 nM, which also shows inhibition in several hormone therapy–sensitive ERb breast cancer xenograft models like MCF7 and HCC1500, as well as three patient-derived primary explant models BR0555, CTC174, and HBCx3. Up to now, AZD2014 enters Phase 1 trial in solid tumours.

Everolimus 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
CAKI1 Cytotoxic Assay 72 h IC50=14 μM 24445311
Colo205 Cytotoxic Assay 72 h IC50=20 μM 24445311
Colo205 Function Assay 24 h Inhibits mTORC1 in human COLO205 cells assessed as reduction of S6 phosphorylation at 0.1 to 8 uM 24836070
Colo205 Function Assay 24 h Inhibits mTORC1 in human COLO205 cells assessed as reduction of 4-EBP1 phosphorylation at 0.1 to 8 uM 24836070

Everolimus 动物研究

Dose Nude Mice: 0.05 mg/kg - 15 mg/kg[2] (p.o.)
Administration p.o.

Everolimus 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.04mL

0.21mL

0.10mL

5.22mL

1.04mL

0.52mL

10.44mL

2.09mL

1.04mL

Everolimus 技术信息

CAS号159351-69-6
分子式C53H83NO14
分子量 958.224
别名 RAD001;SDZ-RAD;Xience V.;Certican;Zortress;Brand name Afinitor;RAD 001.SDZ-RAD
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

溶解度

DMSO: 50 mg/mL(52.18 mM),配合低频超声,并水浴加热至45℃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

动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 3.6 mg/mL clear

PO 0.5% CMC-Na 32 mg/mL suspension

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