WAY-600

WAY-600 Basic information
Product Name:WAY-600
Synonyms:WAY-600;6-(1H-Indol-5-yl)-4-(4-morpholinyl)-1-[1-(3-pyridinylmethyl)-4-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidine;6-(1H-indol-5-yl)-4-morpholino-1-(1-(pyridin-3-ylmethyl)piperidin-4-yl)-1H-pyrazolo[3,4-d]pyrimidine;WAY-600;WAY 600;4-[6-(1H-indol-5-yl)-1-[1-(pyridin-3-ylmethyl)piperidin-4-yl]pyrazolo[3,4-d]pyrimidin-4-yl]morpholine;1H-Pyrazolo[3,4-d]pyrimidine, 6-(1H-indol-5-yl)-4-(4-morpholinyl)-1-[1-(3-pyridinylmethyl)-4-piperidinyl]-;WAY-600 USP/EP/BP
CAS:1062159-35-6
MF:C28H30N8O
MW:494.59
EINECS:
Product Categories:Inhibitors;Akt;mTOR;PI3K;PI3K/Akt/mTOR
Mol File:1062159-35-6.mol
WAY-600 Structure
WAY-600 Chemical Properties
density 1.43
storage temp. Store at -20°C
solubility Soluble in DMSO > 10 mM
form Powder
pka16.08±0.30(Predicted)
Safety Information
MSDS Information
WAY-600 Usage And Synthesis
Biological ActivityWAY-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

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mTORC2

PI3K alpha

1.96 μM (IC 50 )

PI3K gamma

8.45 μM (IC 50 )

WAY-600 Preparation Products And Raw materials
Canertinib Afatinib 7-Bromo-2-(4-hydroxyphenyl)-1,3-benzoxazol-5-ol WAY-151932 N-[4-(2-BROMO-4,5-DIFLUOROPHENOXY)PHENYL]-L-ASPARAGINE MAY-262611 KU-0063794 SAM-315 WAY-204688 WAY 208466 dihydrochloride PELITINIB CYCLOHEXANECARBOXAMIDE, N-[2-[4-(2-METHOXYPHENYL)-1-PIPERAZINYL]ETHYL]-N-2-PYRIDINYL-, HYDROCHLORIDE (1:3) BenzenesulfonaMide, 5-(phenylsulfonyl)-N-4-piperidinyl-2-(trifluoroMethyl)- TENOVIN-1 WYE-354

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