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WYE-125132

Cat. No. M3556
WYE-125132 Structure
Size Price Availability Quantity
5mg USD 220 In stock
10mg USD 300 In stock
50mg USD 750 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Protocol
Cell Experiment
Cell lines WYE-125132
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 Experiment
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
Dosages ≤50 mg/kg
Administration Administered via i.v. or p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 519.6
Formula C27H33N7O4
CAS Number 1144068-46-1
Purity >99%
Solubility DMSO 100 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: WYE-125132 supplier, mTOR, inhibitors

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