美国APExBIO中文官网 - Everolimus (RAD001)

Catalog No. A8169

Everolimus (RAD001)（别名：Everolimus, 依维莫司）

MTOR抑制剂

规格	价格	库存
1mL(10 mM in DMSO)	￥636.00	现货
10mg	￥636.00	现货
25mg	￥1181.00	现货
100mg	￥3181.00	现货

CAS号：159351-69-6纯度：97.37%

仅用于科研，不用于诊疗。未经明确授权不得转售。

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特色产品

Annexin V-FITC/PI Apoptosis Kit

用于双染检测细胞凋亡和坏死

- 在10-20分钟内完成染色
- 适用于流式细胞仪和荧光显微镜检测
- 准确区分活细胞/凋亡细胞/坏死细胞

Phosbind Acrylamide

分离和检测磷酸化/非磷酸化蛋白

- 新型的磷酸盐结合标签和功能分子
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白

Cell Counting Kit-8 (CCK-8)

用于细胞增殖和细胞毒性试验

- 比MTT，MTS或WST-1更敏感
- 对细胞无毒性
- 步骤更简单，无需有机溶剂

Cy5 TSA Fluorescence System Kit

Cy5荧光标记的酪胺信号放大系统

- 检测ICC/IHC/ISH中的低丰度靶点
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率

EZ Cap™ Cy5 Firefly Luciferase mRNA (5-moUTP)

用于观察mRNA运送，定位，翻译

- 具有Cap1结构的荧光素酶mRNA
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰

HotStart™ 2X SYBR Green qPCR Master Mix

用于荧光定量目标DNA或cDNA

- 通过热启动机制优化扩增特异性
- 优异的扩增效率、可重复性和稳定性
- 卓越的灵敏度和准确性，操作简单

HyperScribe™ T7 High Yield Cy5 RNA Labeling Kit Plus

高效的Cy5修饰RNA转录试剂盒

- 适合原位/Northernblot杂交实验
- 优化的缓冲液和T7 RNA聚合酶混合物
- 20 μL反应体系可获得更高的RNA产量

产品描述产品性质产品应用生物相关数据质量控制操作说明产品引用文献摩尔浓度计算器

产品描述

Everolimus (RAD001)是一种有效的和可口服的mTOR抑制剂。mTOR是人类癌症中活性PI3K/Akt通路的一个关键组成部分。Everolimus与mTOR信号通路中的FKBP12受体结合形成everolimus-FKBP12复合体，该复合体进一步与mTOR结合，从而减少下游效应因子S6核糖体蛋白激酶（S6K1）和真核延伸因子4E结合蛋白（4EBP）的活性。除了具有预防器官移植排斥的免疫抑制活性，Everolimus还具有抗肿瘤活性，目前正用于治疗肾细胞癌和其它肿瘤。

参考文献：
G Anandappa, AE Hollingdale, and TG Eisen. Everolimus – a new approach in the treatment of renal cell carcinoma. Cancer Management and Research 2010:2 61-70
Laura Elibenschutz, Delia Colombo, and Caterina Catricala. Everolimus for compassionate use in multiple basal cell carcinomas. Case Reports in Dermatological Medicine 2013
Raffaele Pezzani, Beatrice Rubin, Marco Redaelli, Claudia Radu, Susi Barollo, Maria Verena Cicala, Monica Salva, Caterina Mian, Carla Mucignat-Caretta, Paolo Simioni, Maurizio Iacobone and Franco Mantero. The antiproliferative effects of ouabain and everolimus on adrenocortical tumor cells. Endocrine journal, 2013

产品性质

物理外观	A solid
CAS号	159351-69-6
分子式	C₅₃H₈₃NO₁₄
分子量	958.22
小分子别名	Everolimus
溶解度	≥47.91 mg/mL in DMSO; insoluble in H2O; ≥122 mg/mL in EtOH
SMILES	OCCO[C@H]1[C@H](OC)C[C@H](C[C@H](C)[C@H](CC([C@H](C)/C=C(C)/[C@@H](O)[C@H]2OC)=O)OC([C@@H]3CCCCN3C(C([C@@]4(O)[C@H](C)CC[C@@H](C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C2=O)O4)=O)=O)=O)CC1
存储条件	-20°C
运输条件	蓝冰
SDF文件	Download SDF

产品应用 (实验数据来自文献，APExBIO并未验证，仅供参考)

IC50和靶点

生物活性描述	Everolimus (RAD001)是一种mTOR抑制剂，作用于FKBP12，IC50值为1.6-2.4 nM。
靶点	mTOR (FKBP12)
生物活性数据	1.6-2.4 nM

生物相关数据

质量控制

请选择批次查看:

纯度 = 98.46%

COA (Certificate Of Analysis)HPLC NMR (Nuclear Magnetic Resonance)MSDS (Material Safety Data Sheet)

操作说明

Datasheet

产品引用文献

1. SEOK-HOON JANG, SE HYUN PAEK, et al. "Estrogen Effects Differ Between Medium Maintenance and Replacement from Transcriptional and Clinical Perspectives in T47D Breast Cancer Cells." Anticancer Res. 2023 Oct;43(10):4447-4469. PMID: 37772550
2. Jing Ma, Chao Dong, et al. "Dual Target of EGFR and mTOR Suppress Triple Negative Breast Cancer Cell Growth Via Regulation The Phosphorylation of mTOR Downstream Proteins." Breast Cancer (Dove Med Press). 2023 Jan 17;15:11-24. PMID: 36691572
3. Schwartz, Hannah, et al. "In vitro Methods to Better Evaluate Drug Responses in Cancer." UMass Chan Medical School. September 8, 2022.
4. Narin Ozturk, Dilek Ozturk Civelek, et al. "Dosing-time dependent testicular toxicity of everolimus in mice." Eur J Pharm Sci. 2021 Oct 1;165:105926. PMID: 34242751
5. Silvia-Elena Glont. "Novel insights into the molecular mechanisms of endocrine resistance in ERα positive breast cancer." journal.pone.0215340. April 10, 2019.
6. Syafruddin SE, Rodrigues P, et al. "A KLF6-driven transcriptional network links lipid homeostasis and tumour growth in renal carcinoma." Nat Commun. 2019 Mar 11;10(1):1152. PMID: 30858363
7. Hegab AE, Ozaki M, et al. "Calorie restriction enhances adult mouse lung stem cells function and reverses several ageing-induced changes." J Tissue Eng Regen Med. 2018 Dec 18. PMID: 30562419
8. Wang H, Tian L, et al. "The Osteogenic Niche Is a Calcium Reservoir of Bone Micrometastases and Confers Unexpected Therapeutic Vulnerability." Cancer Cell. 2018 Nov 12;34(5):823-839.e7. PMID: 30423299
9. Hegab AE, Ozaki M, et al. "High fat diet activates adult mouse lung stem cells and accelerates several aging-induced effects." Stem Cell Res. 2018 Oct 4;33:25-35. PMID: 30308415
10. Cheriyan VT, Alsaab H, et al. "A CARP-1 functional mimetic compound is synergistic with BRAF-targeting in non-small cell lung cancers." Oncotarget. 2018 Jul 3;9(51):29680-29697. PMID: 30038713
11. Li J, Zhang J, et al. "Silencing lnc-ASAH2B-2 Inhibits Breast Cancer Cell Growth via the mTOR Pathway." Anticancer Res. 2018 Jun;38(6):3427-3434. PMID: 29848693
12. Ozturk N, Ozturk D, et al. "The immune system as a chronotoxicity target of the anticancer mTOR inhibitor everolimus." Chronobiol Int. 2018 Feb 5:1-14. PMID: 29400578
13. Peng T, Dou QP. "Everolimus Inhibits Growth of Gemcitabine-Resistant Pancreatic Cancer Cells via Induction of Caspase-Dependent Apoptosis and G(2) /M Arrest." J Cell Biochem. 2017 Feb 6. PMID: 28165150