Identification | Back Directory | [Name]
WAY-600 | [CAS]
1062159-35-6 | [Synonyms]
WAY-600 WAY-600;WAY 600 WAY-600 USP/EP/BP 6-(1H-indol-5-yl)-4-morpholino-1-(1-(pyridin-3-ylmethyl)piperidin-4-yl)-1H-pyrazolo[3,4-d]pyrimidine 4-[6-(1H-indol-5-yl)-1-[1-(pyridin-3-ylmethyl)piperidin-4-yl]pyrazolo[3,4-d]pyrimidin-4-yl]morpholine 6-(1H-Indol-5-yl)-4-(4-morpholinyl)-1-[1-(3-pyridinylmethyl)-4-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidine 1H-Pyrazolo[3,4-d]pyrimidine, 6-(1H-indol-5-yl)-4-(4-morpholinyl)-1-[1-(3-pyridinylmethyl)-4-piperidinyl]- | [Molecular Formula]
C28H30N8O | [MDL Number]
MFCD22419019 | [MOL File]
1062159-35-6.mol | [Molecular Weight]
494.59 |
Chemical Properties | Back Directory | [density ]
1.43 | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO > 10 mM | [form ]
Powder | [pka]
16.08±0.30(Predicted) | [color ]
White to off-white |
Hazard Information | Back Directory | [Biological Activity]
WAY-600 is a potent, ATP-competitive, and selective mTOR inhibitor with IC50 of 9 nM for recombinant mTOR enzyme. It blocks mTOR complex 1/2 (mTORC1/2) assembly and activation. | [in vitro]
WAY-600 decreased exhibits a concentration-dependent and time-dependent inhibition of f HepG2 and Huh-7 cells viability. Following WAY-600 (1-1000 nM) treatment, the number of HepG2 cell colonies is dramatically . Meanwhile, BrdU incorporation in HepG2 cells is also inhibited with WAY-600 treatment. It dose-dependently increases the activity of caspase-3 and caspase-9 in HepG2 cells. WAY-600 disrupts assemble of mTORC1 (mTOR-Raptor association ) and mTORC2 (mTOR-Rictor association). Activation of mTORC1 (indicated by p-S6K1 and p-4E-BP1) and mTORC2 is almost blocked by WAY-600 (100 nM). | [in vivo]
Administration of WAY-600 (10 mg/kg, daily) inhibits HepG2 tumor growth in nude mice. Daily HepG2 tumor growth of WAY-600-administrated mice is significantly lower than that of vehicle control mice. Importantly, the in vivo anti-cancer activity by WAY-600 is further potentiated with the co-administration of MEK-162 (2.5 mg/kg, po daily). | [target]
mTOR 9 nM (IC 50 ) | mTORC1 < /span> | mTORC2 | PI3K alpha 1.96 μM (IC 50 ) | PI3K gamma 8.45 μM (IC 50 ) | |
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NCE Biomedical Co.,Ltd.
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