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规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1mL(10 mM in DMSO) | ¥636.00 | 现货 | |
10mg | ¥636.00 | 现货 | |
25mg | ¥1181.00 | 现货 | |
100mg | ¥3181.00 | 现货 |
特色产品
![Cy5 TSA Fluorescence System Kit](/_next/image?url=https%3A%2F%2Fresource.apexbio.cn%2Fapexbio%2Fbanner%2FK1038%EF%BC%8CK1050-K1052_1.png&w=3840&q=75)
- 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)](/_next/image?url=https%3A%2F%2Fresource.apexbio.cn%2Fapexbio%2Fbanner%2FK1079-K1081_1.png&w=3840&q=75)
- 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
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
操作说明
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