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ChemicalBook--->CAS DataBase List--->1062159-35-6

1062159-35-6

1062159-35-6 Structure

1062159-35-6 Structure
IdentificationBack 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 PropertiesBack 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
Spectrum DetailBack Directory
[Spectrum Detail]

WAY-600(1062159-35-6)1HNMR
Hazard InformationBack 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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