Everolimus (RAD001).|159351-69-6|(依维莫司; RAD001; SDZ-RAD)-陌孚医药/Medlife

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Everolimus (RAD001). (Synonyms: 依维莫司; RAD001; SDZ-RAD)

目录号: PC15449 纯度: ≥98%

CAS No. :159351-69-6

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PC15449-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥840.00	请登录

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中文名称

Everolimus (RAD001).

中文别名

依维莫司;依维莫斯;依维莫司溶液;1-哌啶-4-乙酮;Everolimus (RAD001) 抑制剂;呋喃丹高效杀虫剂;依维莫司标准品;依维莫司-[D4]氘代同位素内标;依维莫司Everolimus;依维莫司杂质;EVEROLIMUS依维莫司

英文名称

Everolimus

英文别名

Everolimus;42-O-(2-Hydroxyethyl)-rapamycin;Certica;RAD-001;SDZRAD;Rapamycin, 42-O-(2-hydroxyethyl)-;Certican;CERTICAN(R);Everolimus (RAD001);Everolimus (RAD001, SDZ-RAD, Afinitor®, Certican®, and Zortress®);Everolimus solution; Afinitor;RAD001;SDZ-RAD;Zortress;EVEROLIMUS(WITHOUT BHT);40-O-(2-Hydroxyethyl)rapamycin;42-O-(2-Hydroxyethyl)rapamycin;CERTICAN®;23,27-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine,rapamycin deriv.;42-O-(2-Hydroxy)ethylrapamycin;RAD;XIENCE V;EveroliMus API;Everolimus(RAD001);Votubia;40-O-(2-hydroxyethyl)-rapamycin;Afinitor Disperz;RAD 001;9HW64Q8G6G

Cas No.

159351-69-6

分子式

C₅₃H₈₃NO₁₄

分子量

958.22

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Everolimus (RAD001) is a Rapamycin (HY-10219) derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities.

性状

Solid

IC50 & Target[1][2]

mTOR

5-6 nM (IC₅₀)

体外研究(In Vitro)

Everolimus (RAD001) is an orally active derivative of rapamycin that inhibits the Ser/Thr kinase, mTOR. In both the sensitive murine B16/BL6 melanoma (IC₅₀, 0.7 nM) and the insensitive human cervical KB-31 (IC₅₀, 1,778 nM), antiproliferative concentrations of Everolimus results in total dephosphorylation of S6K1 and the substrate S6 and a shift in the mobility of 4E-BP1, which is indicative of a reduced phosphorylation status. Everolimus exhibits a dose-dependent inhibition in both the total cells and the stem cells from the BT474 cell line and the primary breast cancer cells, albeit with different degrees of growth inhibition. Compare with the total cells, Everolimus is less effective in growth inhibition in the stem cells at all tested concentrations (P<0.001). The IC₅₀ values of Everolimus for BT474 and the primary CSCs are 2,054 and 3,227 nM, or 29 times and 21 times greater than the IC₅₀ values for their corresponding total cells, respectively.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Everolimus is orally active in both mice and rats, producing an antitumor effect that is characterized by dramatic reduction in tumor growth rates as opposed to producing tumor regressions. In the rat CA20498 model, daily treatment with Everolimus (0.5 or 2.5 mg/kg) dose-dependently inhibits growth, and intermittent dosing using a higher dose of 5 mg/kg (once or twice per week) also shows similar antitumor efficacy. Inhibition by Everolimus is characterized by sustained suppression rather than regression and is not associated with any body weight loss. The effect of Everolimus treatment (0.1-10 mg/kg/d) is selective and differ from the effects of PTK/ZK (100 mg/kg). With either growth factor, Everolimus dose-dependently increases the hemoglobin content (convert to blood equivalents and indicative of the number of vessels as well as vascular leakiness) but reduces the Tie-2 content (number of endothelial cells indicative of the number of vessels) and this is significant for VEGF stimulation but not bFGF stimulation. The pharmacokinetics of Everolimus in mice shows that maximum levels of only 0.1 μM are achieved in a human tumor xenograft following a single administration, whereas plasma levels reach 1 to 3 μM for ~4 h.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. OReilly T, et al. Biomarker Development for the Clinical Activity of the mTOR Inhibitor Everolimus (RAD001): Processes,Limitations, and Further Proposals. Transl Oncol. 2010 Apr;3(2):65-79. [Information]

[2]. Kawata T, et al. Dual inhibition of the mTORC1 and mTORC2 signaling pathways is a promising therapeutic target for adult T-cell leukemia. Cancer Sci. 2018 Jan;109(1):103-111. [Information]

[3]. Lane HA, et al. mTOR inhibitor RAD001 (everolimus) has antiangiogenic/vascular properties distinct from a VEGFR tyrosine kinase inhibitor. Clin Cancer Res, 2009, 15(5), 1612-1622. [Information]

[4]. Zhu Y, et al. Antitumor effect of the mTOR inhibitor Everolimus on human breast cancer stem cells 体外研究 and in vivo. Tumour Biol. 2012 Oct;33(5):1349-62. [Information]

溶解度数据

体外研究:

DMSO : 50 mg/mL (52.18 mM; ultrasonic and warming and heat to 60°C)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.0436 mL	5.2180 mL	10.4360 mL
5 mM	0.2087 mL	1.0436 mL	2.0872 mL
10 mM	0.1044 mL	0.5218 mL	1.0436 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (2.61 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (2.61 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (2.61 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (2.61 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (2.61 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (2.61 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
4.

建议依照次序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: 2.5 mg/mL (2.61 mM); Suspended solution; Need ultrasonic
5.

建议依照次序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (2.61 mM); Suspended solution; Need ultrasonic

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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