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| | WYE-687 Basic information |
| Product Name: | WYE-687 | | Synonyms: | methyl 4-(4-morpholino-1-(1-(pyridin-3-ylmethyl)piperidin-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-6-yl)phenylcarbamate;methyl N-[4-[4-morpholin-4-yl-1-[1-(pyridin-3-ylmethyl)piperidin-4-yl]pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]carbamate;WYE-687;WYE 687;WYE687;WYE-687;N-[4-[4-(4-Morpholinyl)-1-[1-(3-pyridinylmethyl)-4-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]carbamic acid methyl ester;N-[4-[4-(4-Morpholinyl)-1-[1-(3-pyridinylmethyl)-4-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-carbamic acid methyl ester hydrochloride;CS-540;Carbamic acid, N-[4-[4-(4-morpholinyl)-1-[1-(3-pyridinylmethyl)-4-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-, methyl ester | | CAS: | 1062161-90-3 | | MF: | C28H32N8O3 | | MW: | 528.61 | | EINECS: | | | Product Categories: | Inhibitors;Akt;PI3K/Akt/mTOR;mTOR;PI3K | | Mol File: | 1062161-90-3.mol |  |
| | WYE-687 Chemical Properties |
| density | 1.40 | | storage temp. | Store at -20°C | | solubility | insoluble in H2O; insoluble in EtOH; insoluble in DMSO | | form | Powder | | pka | 13.42±0.70(Predicted) |
| | WYE-687 Usage And Synthesis |
| Uses | WYE-687 is an ATP-competitive and selective inhibitor of mammalian target of rapamycin (mTOR). Studies have shown the combination of Ras-Raf-MEK1/2 inhibitors with WYE-687 may overcome resistance to m
TorKIs thus may be an effective additive therapy for treatment of patient with renal cell carcinoma or colorectal cancer. | | Uses | WYE-687 is an ATP-competitive and selective inhibitor of mammalian target of rapamycin (mTOR). Studies have shown the combination of Ras-Raf-MEK1/2 inhibitors with WYE-687 may overcome resistance to mTorKIs thus may be an effective additive therapy for treatment of patient with renal cell carcinoma or colorectal cancer. | | Biological Activity | wye-687 is an atp-competitive inhibitor of mtor with ic50 value of 7nm [1].wye-687 is a small-molecule pyrazolopyrimidine inhibitor of mtor1 and mtor2. in the immune-complex kinase assay using his6-akt and his6-s6k as the specific substrates of mtor1 and mtor2, wye-687 prevents mtor from phosphorylating the substrates dose-dependently. besides that, wye-687 is found to highly selective against pi3kα (>100-fold) and pi3kγ (>500-fold) as well as 24 other protein kinases. it is found that wye-687 can suppress cell growth via causing a strong g1 arrest in cell cycle in tumor cell lines including mda361 and hct116. wye-687 also affects the angiogenic factor of cancer cells. it reduces the expression of hif-1α in u87mg, mda361 and lncap cells [1]. | | references | [1] yu k, toral-barza l, shi c, et al. biochemical, cellular, and in vivo activity of novel atp-competitive and selective inhibitors of the mammalian target of rapamycin. cancer research, 2009, 69(15): 6232-6240. |
| | WYE-687 Preparation Products And Raw materials |
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