Everolimus (RAD001)

Catalog No. A10374

Everolimus (RAD001)是西罗莫司的40-O-(2-羟乙基)衍生物，与西罗莫司作为mTOR抑制剂的作用相似。

Product Citations

Ming-Chun Hung, .et al. AKT phosphorylation as a predictive biomarker for PI3K/mTOR dual inhibition-induced proteolytic cleavage of mTOR companion proteins in small cell lung cancer, Cell Biosci, 2022, 12: 122 PMID: 35918763
Yusuke Murase, .et al. Antitumor activity of the dual PI3K/mTOR inhibitor gedatolisib and the involvement of ABCB1 in gedatolisib resistance in canine tumor cells, Oncol Rep, 2022, Apr;47(4):61 PMID: 35088890
Gabriela Torres-Flores, .et al. Preparation and Characterization of Liposomal Everolimus by Thin-Film Hydration Technique, Adv Polym Technol, 2020, ID 5462949
Takaaki Fujimura, .et al. Enhanced antitumor effect of alectinib in combination with cyclin-dependent kinase 4/6 inhibitor against RET-fusion-positive non-small cell lung cancer cells, Cancer Biol Ther, 2020, Sep 1;21(9):863-870 PMID: 32835580
BD Henriksbo, .et al. Statins Activate the NLRP3 Inflammasome and Impair Insulin Signaling via p38 and mTOR, Am J Physiol Endocrinol Metab, 2020, Jul 1;319(1):E110-E116 PMID: 32421368
Hiroshi Fukamachi, .et al. A subset of diffuse-type gastric cancer is susceptible to mTOR inhibitors and checkpoint inhibitors, J Exp Clin Cancer Res, 2019, 38:127 PMID: 30866995
Nachi Namatame, .et al. Antitumor profile of the PI3K inhibitor ZSTK474 in human sarcoma cell lines, Oncotarget, 2018, Oct 12; 9(80): 35141-35161 PMID: 30416685
Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
Rieko Ohki, .et al. PHLDA3 is a novel tumor suppressor of pancreatic neuroendocrine tumors, Proc Natl Acad Sci U S A, 2014, 111(23): E2404-E2413 PMID: 24912192

Technical details

Catalog Num	A10374
M. Wt	958.2
Formula	C53H83NO14
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	159351-69-6
Synonyms	SDZ-RAD, Certican, Zortress, Afinitor
SMILES	C[C@@H]1CC[C@H]2C[C@@H](/C(=C/C=C/C=C/[C@H](C[C@H](C(=O)[C@@H]([C@@H](/C(=C/[C@H](C(=O)C[C@H](OC(=O)[C@@H]3CCCCN3C(=O)C(=O)[C@@]1(O2)O)[C@H](C)C[C@@H]4CC[C@H]([C@@H](C4)OC)OCCO)C)/C)O)OC)C)C)/C)OC

Biological Activity

Everolimus (RAD001)是西罗莫司的40-O-(2-羟乙基)衍生物，与西罗莫司作为mTOR抑制剂的作用相似。

Targets

mTOR (FKBP12) (Cell-free assay)
1.6 nM-2.4 nM

Solubility *

In vitro (25°C)	DMSO	91 mg/mL (94.97 mM)
	Water	Insoluble
	Ethanol	6 mg/mL (6.26 mM)
In vivo	30% Propylene glycol (dissolve first)+5% Tween 80+ddH2O	4 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	10.44 mL	52.18 mL	104.36 mL
0.5 mM	2.09 mL	10.44 mL	20.87 mL
1 mM	1.04 mL	5.22 mL	10.44 mL
5 mM	0.21 mL	1.04 mL	2.09 mL

*The above data is based on the productmolecular weight 958.2 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.