Everolimus (RAD001)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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
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- 3. 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
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Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 958.22 |
Cas No. | 159351-69-6 |
Formula | C53H83NO14 |
Synonyms | Everolimus, RAD001 |
Solubility | ≥47.91 mg/mL in DMSO; insoluble in H2O; ≥122 mg/mL in EtOH |
SDF | Download SDF |
Canonical 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 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验[1]: | |
细胞系 |
胰腺癌细胞系Panc-1和小细胞肺癌细胞系SCLC |
溶解方法 |
在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
24 h;IC50:50 μg/mL(Panc-1);5 μg/mL(SCLC)。 |
应用 |
Everolimus具有抗增殖活性。在Panc-1和SCLC中,everolimus剂量依赖地抑制BrdU的掺入,IC50值分别为50 μg/mL和5 μg/mL,两者都是高浓度,在人体中是不可行的。Everolimus用于治疗的血清水平介于0.005和0.01 μg/mL之间。 |
动物实验[2]: | |
动物模型 |
卵巢癌TgMISIIR-TAg-DR26小鼠模型 |
剂量 |
RAD001溶解在2%(重量/体积)的微乳液中,口服灌胃之前在双蒸水中稀释。安慰剂(对照)或5 mg/kg RAD001以口服方式每周给药两次,在小鼠5周龄时开始,一直持续到20周。安慰剂或RAD001处理的小鼠用MRM扫描。 |
应用 |
RAD001抑制肿瘤发生。RAD001处理小鼠的体重比安慰剂处理小鼠低约10%。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1] Stracke S, Ramudo L, Keller F, et al. Antiproliferative and overadditive effects of everolimus and mycophenolate mofetil in pancreas and lung cancer cells in vitro. Transplantation proceedings. Elsevier, 2006, 38(3): 766-770. [2] Mabuchi S, Altomare D A, Connolly D C, et al. RAD001 (Everolimus) delays tumor onset and progression in a transgenic mouse model of ovarian cancer. Cancer Research, 2007, 67(6): 2408-2413. |
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) | |||||
IC50 | 1.6-2.4 nM |
质量控制和MSDS
- 批次: