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WYE-354

Cat. No. M1755
WYE-354 Structure
Size Price Availability Quantity
10mg USD 165 In stock
50mg USD 620 In stock
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Quality Control
Biological Activity

WYE-354 is a potent and ATP competitive inhibitor of mTOR (IC50 = 5 nM), with significant selectivity over PI3K isofoms (>100-fold). WYE-354 is equally potent against mTORC1 and mTORC2 activities in HEK293 immune complex kinase assays using S6K and Akt as the respective substrate (IC50 <200 nM) and effectively blocks cellular phosphorylation of S6K on T389 and Akt on S473 both in cultures and in a murine xenograft model, resulting in a significant suppression of PC3MM2-derived tumor growth (by 86% on day 7; 50 mg/kg, i.p twice per day) in vivo.

Protocol
Cell Experiment
Cell lines Cell lines of Rat1, HEK293, MDA-MB-361, MDA-MB-468, MDA-MB-231, LNCap, DU145, U87MG, A498, HCT116, and HT29
Preparation method Tumor cell growth assays.
Concentrations 0~100 μ M
Incubation time 3 days
Animal Experiment
Animal models PC3MM2 tumors xenograft in BALB/c nu/nu female mice
Formulation formulated in 5% ethanol, 5% polysorbate 80, 5% polyethylene glycol-400
Dosages a single i.p. injection with 50 mg/kg
Administration i.p.
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 495.5
Formula C24H29N7O5
CAS Number 1062169-56-5
Purity 100.00%
Solubility DMSO
Storage at -20°C
References

Inhibition of mTORC1 kinase activates Smads 1 and 5 but not Smad8 in human prostate cancer cells, mediating cytostatic response to rapamycin.
Wahdan-Alaswad RS et al. Mol Cancer Res. 2012 Jun;10(6):821-33. PMID: 22452883.

Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin.
Yu K et al. Cancer Res. 2009 Aug 1;69(15):6232-40. PMID: 19584280.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: WYE-354 supplier, mTOR, inhibitors

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