Home > Products > PI3K/Akt/mTOR > mTOR > Everolimus

Everolimus

(CAS No:159351-69-6)

Everolimus (RAD001) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay.

CAS No:159351-69-6

Molecular Weight(MW):958.22

Purity:99.00%

Specification:500MG;1G;5G;10G;50G;100G

Price and large packaging, please e-mail consultation:info@SuperLan-chem.com

QC Documents

COA	MSDS	HPLC	NMR

ChemicalInfomation

CAS No:	159351-69-6
Molecular formula(MF)	C₅₃H₈₃NO₁₄
Molecular Weight(MW):	958.22
Alias	42-O-(2-Hydroxyethyl)-rapamycin;Certica;RAD-001;SDZRAD;Rapamycin, 42-O-(2-hydroxyethyl)-;Everolimus;Certican;CERTICAN(R)

Solubility

In vitro	DMSO	100 mg/mL (104.36 mM)
	Ethanol	7 mg/mL (7.3 mM)
	Water	<1 mg/mL
In vivo	30% Propylene glycol (dissolve first)+5% Tween 80+ddH2O	5mg/mL

Biological Activity

Description

Everolimus (RAD001) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay.

Targets

mTOR (FKBP12) ^[1]
(Cell-free assay)

1.6 nM-2.4 nM

In vitro

Everolimus exhibits the immunosuppressive activity which is comparable to that of rapamycin. Everolimus competes with immobilized FK 506 for binding to biotinylated FKBP12 and shows the inhibitory effect on a two-way MLR performed with spleen cells from BALB/c and CBA mice with IC50 of 0.12-1.8 nM. ^[1] Everolimus also shows antiangiogenic/vascular effects in VEGF-induced HUVEC proliferation with IC50 of 0.12 nM and bFGF-induced HUVEC proliferation with IC50 of 0.8 nM, respectively. ^[2] A recent study shows that Everolimus shows a dose-dependent inhibitory effects on both the total cells and the stem cells from the BT474 cell line and the primary breast cancer cells with IC50 of 156 nM in total cells of primary breast cancer cells and 71 nM in total cells of BT474 cells. In addition, combination treatment with Everolimus and trastuzumab produces the significantly increased inhibition on the growth of cancer stem cells with the inhibition rate increased by more than 50 %. ^[3]

Cell Data

Cell Lines	Assay Type	Incubation Time	Formulation	Activity Description	PMID
SQ20B	Cytotoxic Assay	72 h	DMSO	IC50=5.5 Î¼M	24445311
Colo205	Cytotoxic Assay	72 h	DMSO	IC50=20 Î¼M	24445311
ColoR	Cytotoxic Assay	72 h	DMSO	IC50=8.7 Î¼M	24445311
HCT116	Cytotoxic Assay	72 h	DMSO	IC50=12 Î¼M	24445311
HT29	Cytotoxic Assay	72 h	DMSO	IC50=15 Î¼M	24445311
CAKI1	Cytotoxic Assay	72 h	DMSO	IC50=14 Î¼M	24445311
SK-HEP1	Cytotoxic Assay	72 h	DMSO	IC50=12 Î¼M	24445311
DU145	Cytotoxic Assay	72 h	DMSO	IC50=8 Î¼M	24445311
OVCAR3	Cytotoxic Assay	72 h	DMSO	IC50=16 Î¼M	24445311
HOP62	Cytotoxic Assay	72 h	DMSO	IC50=19 Î¼M	24445311
Colo205	Function Assay	24 h	DMSO	Inhibits mTORC1 in human COLO205 cells assessed as reduction of S6 phosphorylation at 0.1 to 8 uM	24836070
Colo205	Function Assay	24 h	DMSO	Inhibits mTORC1 in human COLO205 cells assessed as reduction of 4-EBP1 phosphorylation at 0.1 to 8 uM	24836070
SK-HEP1	Function Assay	24 h	DMSO	Inhibits mTORC1 in human SK-HEP1 cells assessed as reduction of S6 phosphorylation at 0.1 to 8 uM	24836070
SK-HEP1	Function Assay	24 h	DMSO	Inhibits mTORC1 in human SK-HEP1 cells assessed as reduction of 4-EBP1 phosphorylation at 0.1 to 8 uM	24836070

... Click to View More Cell Line Experimental Data

In vivo

Everolimus (0.1 to 10 mg/kg) dose-dependently inhibits growth of the primary (ear) and lymph node metastases of B16/BL6 melanoma, with decreased total number of vessels and reduced mature vessels. ^[2] In a xenograft animal model of BT474 stem cells, Everolimus shows significant reductions in mean tumor sizes (590.6 mm³), compared to the control group with a tumor size of 698 mm³. Furthermore, combination treatment with Everolimus and trastuzumab significantly decreases the xenograft tumor size (410.8 mm³) more than Everolimus treatment alone. ^[3]