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WYE-354 Chemical Structure
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Biological Activity
WYE-354,a cell-permeable pyrazolopyrimidine compound,is a potent and ATP competitive inhibitor of mTOR (IC50 = 5 nM), with significant selectivity over PI3K isofoms (>100-fold). When injected into tumor-bearing nude mice, WYE-354 inhibited mTORC1 and mTORC2 and displayed robust antitumor activity in PTEN-null tumors. [1]
References on WYE-354
- [] Cancer Res 2009;69:6232-6240
Chemical Information
| Molecular Weight (WM): | 495.53 |
|---|---|
| Formula: | C24H29N7O5 |
| CAS No.: | 1062169-56-5 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥99mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
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Click to enlarge
For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of WYE-354 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan.
For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of WYE-354 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan.
Data independently produced by Dr. Yong-Weon Yi from Georgetown University Medical Center.WYE-354 purchased from Selleck. WYE-354 purchased from Selleck
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Click to enlarge
HCT116 were left untreated (C) or stimulated for 5 h with serum (FBS) and rapamycin or WYE-354 at the indicated concentrations.
HCT116 were left untreated (C) or stimulated for 5 h with serum (FBS) and rapamycin or WYE-354 at the indicated concentrations.
Data independently produced by Dr. Pierre P. Roger from Free University of Brussels. WYE-354 purchased from Selleck
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Click to enlarge
After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of WYE-354 for 3h,followed by 20-minute stimolation of 100ng/ml EGF. - After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of WYE-354 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
Data independently produced by Dr. Zhang of Tianjin Medical University WYE-354 purchased from Selleck
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For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of WYE-354 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan. |
Data independently produced by Dr. Yong-Weon Yi from Georgetown University Medical Center.WYE-354 purchased from Selleck.
HCT116 were left untreated (C) or stimulated for 5 h with serum (FBS) and rapamycin or WYE-354 at the indicated concentrations. |
Data independently produced by Dr. Pierre P. Roger from Free University of Brussels.
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