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Everolimus

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产品编号 T1784Cas号 159351-69-6
别名 依维莫司, SDZ-RAD, RAD001

Everolimus (SDZ-RAD) 是 Rapamycin 的衍生物,是一种 mTOR1 抑制剂,具有选择性和口服活性。Everolimus 具有免疫抑制和抗肿瘤活性,可以抑制肿瘤细胞增殖、诱导细胞凋亡和自噬。

Everolimus

Everolimus

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纯度: 99.52%
产品编号 T1784 别名 依维莫司, SDZ-RAD, RAD001Cas号 159351-69-6

Everolimus (SDZ-RAD) 是 Rapamycin 的衍生物,是一种 mTOR1 抑制剂,具有选择性和口服活性。Everolimus 具有免疫抑制和抗肿瘤活性,可以抑制肿瘤细胞增殖、诱导细胞凋亡和自噬。

规格价格库存数量
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 x 10 mM (in DMSO)¥ 589现货
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产品介绍

生物活性
产品描述
Everolimus (SDZ-RAD) is a derivative of Rapamycin, an mTOR1 inhibitor with selective and oral activity. Everolimus exhibits immunosuppressive and antitumor activity, inhibiting tumor cell proliferation, inducing apoptosis and autophagy.
靶点活性
mTOR FKBP12:1.6-2.4 nM (cell free)
体外活性
方法:原发性乳腺癌细胞和 BT474 细胞用 Everolimus (0.001-10 µM) 处理 24 h,使用 MTT assay 检测细胞活力。
结果:Everolimus 对原发性乳腺癌细胞和 BT474 细胞具有剂量依赖性抑制作用,IC 50 分别为 156 nM 和 71 nM。[1]
方法:乳腺癌细胞 MCF-7 和 BT474 用 Everolimus (5 mg/mL) 处理 48 h,使用 Flow cytometry 检测细胞凋亡情况。
结果:Everolimus 在孵育 48 h 后诱导 MCF-7 和 BT474 细胞的凋亡。[2]
体内活性
方法:为测试体内抗肿瘤活性,将 Everolimus (5-10 mg/kg in 0.5% CMC) 灌胃给药给携带乳腺癌肿瘤 MC4-L2 的 BALB/c 小鼠,每周五次,持续二十天。
结果:10 mg/kg 和 5 mg/kg 剂量的 Everolimus 都能有效抑制肿瘤生长,从而减少乳腺肿瘤体积。[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, SDZ-RAD, RAD001
化学信息
分子量958.22
分子式C53H83NO14
CAS No.159351-69-6
Smiles[H][C@@]12CC[C@@H](C)[C@@](O)(O1)C(=O)C(=O)N1CCCC[C@@]1([H])C(=O)O[C@@]([H])(CC(=O)[C@H](C)\C=C(C)\[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)\C=C\C=C\C=C(C)\[C@H](C2)OC)[C@H](C)C[C@@H]1CC[C@@H](OCCO)[C@@H](C1)OC
密度1.18 g/cm3
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (5.22 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
Ethanol: 50 mg/mL
DMSO: 50 mg/mL (52.18 mM)
H2O: Insoluble
溶液配制表
1mg5mg10mg50mg
1 mM1.0436 mL5.2180 mL10.4360 mL52.1801 mL
5 mM0.2087 mL1.0436 mL2.0872 mL10.4360 mL
1mg5mg10mg50mg
10 mM0.1044 mL0.5218 mL1.0436 mL5.2180 mL
20 mM0.0522 mL0.2609 mL0.5218 mL2.6090 mL
50 mM0.0209 mL0.1044 mL0.2087 mL1.0436 mL

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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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
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2 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。
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