产品说明书

Everolimus

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Chemical Structure| 159351-69-6 同义名 : RAD001;SDZ-RAD;Xience V.;Certican;Zortress;Brand name Afinitor;RAD 001.SDZ-RAD
CAS号 : 159351-69-6
货号 : A116645
分子式 : C53H83NO14
纯度 : 99%+
分子量 : 958.224
MDL号 : MFCD00929329
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: 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

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.
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
实验方案
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