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Everolimus

产品编号 T1784 CAS 159351-69-6

别名: 依维莫司, RAD001, SDZ-RAD

Everolimus (SDZ-RAD) 是 Rapamycin 的衍生物，也是一种口服活性的mTOR1选择性抑制剂。它与FKBP-12结合可产生免疫抑制复合物，还抑制肿瘤细胞增殖并诱导细胞凋亡和自噬，有免疫抑制和抗癌活性。

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Everolimus, CAS 159351-69-6

规格	价格/CNY	货期
1 mg	￥ 196	现货
5 mg	￥ 435	现货
10 mg	￥ 655	现货
25 mg	￥ 1,250	现货
50 mg	￥ 2,190	现货
100 mg	￥ 3,520	现货
200 mg	￥ 4,280	现货
1 g	￥ 6,590	现货
1 mL * 10 mM (in DMSO)	￥ 589	现货

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选择批次

纯度: 99.52%

纯度: 99.48%

纯度: 98.66%

纯度: 98%

纯度: 97.76%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Everolimus (SDZ-RAD) is a potent mTOR inhibitor that binds to FKBP-12. It is used alone or in combination with calcineurin inhibitors.
靶点活性	mTOR FKBP12:1.6-2.4 nM (cell free)
体外活性	Everolimus competes with immobilized FK 506 for binding to biotinylated FKBP12 (IC50: 0.12-1.8 nM) [1]. RAD001 inhibited proliferation in vitro (IC50 values<1 nM to >1 μM), and pS6 kinase and 4E-BP1 were inhibited. In vitro, RAD001 inhibited the proliferation of VEGF-stimulated and fibroblast growth factor-stimulated human endothelial cells [2]. Everolimus exhibited a dose-dependent inhibition in both the total cells and the stem cells from the BT474 cell line and the primary breast cancer cells. The IC50 values of everolimus for BT474 and the primary CSCs were 2,054 and 3,227 nM, or 29 times and 21 times greater than the IC50 values for their corresponding total cells, respectively [3].
体内活性	In vivo, in tumor models derived from either sensitive or insensitive cells, RAD001 reduced Tie-2 levels, the amount of mature and immature vessels, total plasma, and tumor VEGF. RAD001 did not affect blood vessel leakiness in normal vasculature acutely exposed to VEGF nor did it affect tumor vascular permeability[2]. Compared to the control group, the everolimus, trastuzumab, and drug combination groups showed significant reductions in mean tumor sizes. Compared to the mean xenograft tumor size in the trastuzumab group, the mean tumor size in the everolimus group was larger. When the two drugs were combined, the xenograft tumor size was smaller than those of the groups treated with everolimus or trastuzumab alone [3].
激酶实验	Binding to the FK 506 binding protein (FKBP12) was indirectly assessed by means of an ELISA-type competition assay. FK 506 was included in each individual experiment as a standard, and the inhibitory activity is expressed as relative IC50 compared to FK 506 (rIC50 5 IC50 test compound/IC50 FK 506). Details regarding this assay have been reported [1].
细胞实验	BT474 stem cells that were sorted by flow cytometry were cultured in stem cell culture medium in 25-ml cell culture flasks. The cells were divided into four groups: (1) the control group (blank control), (2) the Ever group (100 nM everolimus), (3) the Tz group (10 μg/ml trastuzumab), and (4) the Ever+Tz group (100 nM everolimus and 10 μg/ml trastuzumab). Culture medium with 0.5 % DMSO was added to the blank control group. After treatment, the cells were cultured in an incubator at 37 °C with 5 % CO2 for 24 h before the cells were collected. For cell cycle determination, the cells in the different treatment groups were fixed in ice-cold ethanol for 24 h. The ethanol was removed, 500 μl RNase-containing propidium iodide (PI) and 1 mL PBS were added, and the cells were incubated at 4 °C for 30–60 min in the dark. The samples were then sorted by flow cytometry according to each cell cycle stage, and G0/G1 %, S%, and G2/M% were calculated to obtain the cell cycle distribution. To understand the effect of drug treatment on stem cell apoptosis, annexin-FITC and PI were added to the single-cell suspension and mixed well before incubation at room temperature for 5–15 min in the dark. The cells were then sorted by flow cytometry within 1 h after incubation to measure the rate of apoptosis [3].
动物实验	Cultured BT474 stem cells were collected and pelleted by centrifugation at 1,000 rpm for 5 min. The cells were then washed with serum- and antibiotics-free DMEM medium three times. After the cells were counted, aliquots of cells at 1×10^5/100 μl in serum- and antibiotic-free culture medium in (microcentrifuge tubes) were sent to the animal room under sterile conditions. A volume of 100 μl stem cell suspension was injected beneath the left breast pad of BALB/c nude mice. The injected mice were housed in clean cages under a constant temperature of 20–25 °C with free access to food and water. When the tumor volume was approximately 300 mm3 (approximately 9 days after stem cell injection), the tumor-bearing mice were randomly divided into four groups (five animals/group): (1) the control group (normal saline), (2) the Ever group (2 mg/kg everolimus), (3) the Tz group (5 mg/kg trastuzumab), and (4) the Ever+Tz group (2 mg/kg everolimus and 5 mg/kg trastuzumab); this day was denoted as day 1. Thereafter, the greatest longitudinal diameter (L) and the greatest transverse diameter (W) of the xenograft tumors in mice were measured by caliper in the morning once every 3 days, and tumor volumes were calculated and recorded when the test articles were administered. After the last tumor volume measurement on day 16, the mice were euthanized by cervical dislocation, and tumor specimens were collected and fixed for histochemical assays [3].

别名	依维莫司, RAD001, SDZ-RAD
化合物与蛋白结合的复合物	Cytochrome P450 107G1 (RapN) with everolimus
分子量	958.22
分子式	C53H83NO14
CAS No.	159351-69-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 50 mg/mL

DMSO: 50 mg/mL (52.18 mM)

H2O: Insoluble

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.0436 mL	5.218 mL	10.436 mL	26.09 mL
	5 mM	0.2087 mL	1.0436 mL	2.0872 mL	5.218 mL
	10 mM	0.1044 mL	0.5218 mL	1.0436 mL	2.609 mL
	20 mM	0.0522 mL	0.2609 mL	0.5218 mL	1.3045 mL
	50 mM	0.0209 mL	0.1044 mL	0.2087 mL	0.5218 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

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参考文献

1. Sedrani R, et al. Chemical modification of rapamycin: the discovery of SDZ RAD. Transplant Proc. 1998 Aug;30(5):2192-4. 2. Lane HA, et al. mTOR inhibitor RAD001 (everolimus) has antiangiogenic/vascular properties distinct from a VEGFR tyrosine kinase inhibitor. Clin Cancer Res. 2009 Mar 1;15(5):1612-22. 3. Zhu Y, et al. Antitumor effect of the mTOR inhibitor everolimus in combination with trastuzumab on human breast cancer stem cells in vitro and in vivo. Tumour Biol. 2012 Oct;33(5):1349-62.

文献引用

1. Nian Z, Zheng X, Dou Y, et al. Rapamycin pretreatment rescues the bone marrow AML cell elimination capacity of CAR-T cells. Clinical Cancer Research. 2021 2. Sun R, Ge W, Zhu Y, et al.Proteomic Dynamics of Breast Cancer Cell Lines Identifies Potential Therapeutic Protein Targets.Molecular & Cellular Proteomics.2023: 100602. 3. Dong S, Matossian M D, Yousefi H, et al.Targeting Mcl-1 by a small molecule NSC260594 for triple-negative breast cancer therapy.Scientific Reports.2023, 13(1): 11843. 4. Hong J H, Yong C H, Heng H L, et al.Integrative multiomics enhancer activity profiling identifies therapeutic vulnerabilities in cholangiocarcinoma of different etiologies.Gut.2023

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Everolimus 159351-69-6 Apoptosis Autophagy Others PI3K/Akt/mTOR signaling mTOR inhibit 依维莫司 FK506-binding protein RAD001 RAD 001 SDZ-RAD Mammalian target of Rapamycin RAD-001 FKBP Inhibitor inhibitor

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Everolimus

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

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剂量换算

体内实验配液计算器

技术支持

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