WYE-125132 is a highly potent, ATP-competitive and specific mTOR kinase inhibitor with an IC50 of 0.19 nM. WYE-125132 blocked the activity of the both of mTORC1 and mTORC2 in various models of cancer in vitro and in vivo. WYE-125132 is 5,000-fold more selective than PI3Ks. Moreover, WYE-125132 completely blocked amino acid-induced phosphorylation of Maf1, just as S6K1, and 4E-BP1 via the inhibition of mTOR. WYE-132-treated MG63 markedly upregulated the Maf1 amouts in the nucleus. WYE-125132 showed a substantially more effective inhibition in many respects, including cancer cell growth and survival, protein synthesis bioenergetic metabolism, and adaptation to hypoxia by contrast with the rapalog temsirolimus/CCI-779.
|Preparation method||Obtaining cell lines of MDA-MB-361, MDA-MB-231, MDA-MB-468, BT549, LNCap, A549, H1975, H157, H460, U87MG, A498, 786-O, HCT116, MG63, Rat1, HEK293, and HeLa from the American Type Culture Collection. Describing cell growth assays and IC50 determination as follows. For tumor cell growth assays, plating cells in 96-well culture plates at 1000 to 3000 cells per well for 24 hours, treating with DMSO or various doses of WYE-125132. Viable cell densities are determined three days later by MTS assay employing an assay kit following the kit assay protocol.Calculating the effect of each treatment as percent of control growth relative to the DMSO-treated cells grown in the same culture plate. Ploting inhibitor dose response curves for determination of IC50 values.|
|Concentrations||0 to 10 μM|
|Incubation time||24 hours|
|Animal models||U87MG, MDA361, H1975, A549, A498, and 786-O cells are injected s.c. into the right flank of CD1 nu/nu mice|
|Formulation||WYE-125132 is dissolved in 5% ethanol, 2% Tween 80, and 5% polyethylene glycol-400|
|Administration||Administered via i.v. or p.o.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 100 mg/mL|
|Related mTOR Products|
CZ415 是一种有效的高选择性 mTOR 抑制剂。
GNE-477 is a potent and efficacious dual PI3K (IC50=4 nM)/mTOR(Ki=21 nM) inhibitor.
Zotarolimus (ABT-578) is an analogue of rapamycin, and inhibits FKBP-12 binding with IC50 of 2.8 nM.
LY303511 is a structural analogue of LY294002, which does not inhibit PI3K, increased homotypic GJIC.
Temsirolimus (CCI-779) is a specific mTOR inhibitor with IC50 of 1.76 μM.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.