ChemicalBook--->CAS DataBase List--->1062161-90-3

1062161-90-3

1062161-90-3 Structure

1062161-90-3 Structure
IdentificationBack Directory
[Name]

WYE-687
[CAS]

1062161-90-3
[Synonyms]

CS-540
WYE-687
WYE-687 USP/EP/BP
WYE-687;WYE 687;WYE687
17α-Ethynyltestosterone
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
N-[4-[4-(4-Morpholinyl)-1-[1-(3-pyridinylmethyl)-4-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]carbamic acid methyl ester
Carbamic acid, N-[4-[4-(4-morpholinyl)-1-[1-(3-pyridinylmethyl)-4-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-, 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
[Molecular Formula]

C28H32N8O3
[MDL Number]

MFCD22417086
[MOL File]

1062161-90-3.mol
[Molecular Weight]

528.61
Chemical PropertiesBack Directory
[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)
[color ]

Off-white to yellow
Hazard InformationBack Directory
[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].
[storage]

Store at -20°C
[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.
Spectrum DetailBack Directory
[Spectrum Detail]

WYE-687(1062161-90-3)1HNMR
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