All AbMole products are for research use only, cannot be used for human consumption.
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.
 |
Source | Oncotarget (2015). Figure 1. WYE-354 |
| Method | MTS assay | |
| Cell Lines | Western blot analysis | |
| Concentrations | 1 μM | |
| Incubation Time | 24, 48, and 72 h | |
| Results | WYE-354 significantly reduced cell viability starting at a 1 μM concentration after a 24 hours exposure, in both studied cell lines |
| 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. |
| Molecular Weight | 495.5 |
| Formula | C24H29N7O5 |
| CAS Number | 1062169-56-5 |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related mTOR Products |
|---|
| RMC-4627
RMC-4627 is a selective mTORC1 inhibitor that activates 4EBP1 and inhibits tumor growth. |
| RMC-4529
RMC-4529 has an IC50 value of 1.0 nM against p-4E-BP1-(T37/46) in mTOR kinase cellular assay. |
| WYE-687 dihydrochloride
WYE-687 dihydrochloride is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. |
| Rapamycin-d3
Rapamycin-d3 |
| L-Leucine-d10
L-Leucine-d10 |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
