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WAY-600

Basic information Safety Supplier Related

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
  • 4-(6-(1H-Indol-5-yl)-1-(1-(pyridin-3-ylmethyl)piperidin-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)morpholine
CAS:
1062159-35-6
MF:
C28H30N8O
MW:
494.59
Product Categories:
  • Inhibitors
  • Akt
  • mTOR
  • PI3K
  • PI3K/Akt/mTOR
Mol File:
1062159-35-6.mol
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WAY-600 Chemical Properties

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
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WAY-600 Usage And Synthesis

Uses

WAY-600 is a potent, ATP-competitive, and selective mTOR inhibitor with an IC50 of 9 nM for recombinant mTOR enzyme. WAY-600 blocks mTOR complex 1/2 (mTORC1/2) assemble and activation.

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

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mTORC2

PI3K alpha

1.96 μM (IC 50 )

PI3K gamma

8.45 μM (IC 50 )

IC 50

mTOR: 9 nM (IC50); mTORC1; mTORC2; PI3K alpha: 1.96 μM (IC50); PI3K gamma: 8.45 μM (IC50)

References

[1] Yu K, et al. Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin. Cancer Res. 2009 Aug 1;69(15):6232-40. DOI:10.1158/0008-5472.CAN-09-0299
[2] Wang K, et al. MEK-ERK inhibition potentiates WAY-600-induced anti-cancer efficiency in preclinical hepatocellular carcinoma (HCC) models. Biochem Biophys Res Commun. 2016 May 27;474(2):330-7. DOI:10.1016/j.bbrc.2016.04.099

WAY-600Supplier

Jinan Trio PharmaTech Co., Ltd.
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0531-88811783
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sales@trio-pharmatech.com
NCE Biomedical Co.,Ltd.
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4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Shanghai Aladdin Bio-Chem Technology Co.,LTD
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400-6206333 13167063860
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anhua.mao@aladdin-e.com
MedChemexpress LLC
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021-58955995
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AdooQ BioScience, LLC
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+1 (866) 930-6790
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info@adooq.com
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WAY-600(1062159-35-6)Related Product Information