CAS 1062159-35-6|WAY-600

Introduction:Basic information about CAS 1062159-35-6|WAY-600, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameWAY-600
CAS Number1062159-35-6Molecular Weight494.591
Density1.4±0.1 g/cm3Boiling Point678.1±55.0 °C at 760 mmHg
Molecular FormulaC28H30N8OMelting Point/
MSDS/Flash Point363.9±31.5 °C

Names

Name4-[6-(1H-indol-5-yl)-1-[1-(pyridin-3-ylmethyl)piperidin-4-yl]pyrazolo[3,4-d]pyrimidin-4-yl]morpholine
SynonymMore Synonyms

WAY-600 BiologicalActivity

DescriptionWAY-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.
Related CatalogResearch Areas >>CancerResearch Areas >>Inflammation/Immunology
Target

mTOR:9 nM (IC50)

mTORC1

mTORC2

PI3K alpha:1.96 μM (IC50)

PI3K gamma:8.45 μM (IC50)

In VitroWAY-600 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 decreased. Meanwhile, BrdU incorporation in HepG2 cells is also inhibited with WAY-600 treatment. WAY-600 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)[2].
In VivoAdministration 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, p.o. daily)[2].
Cell AssayEstablished HCC cells (HepG2 and Huh-7), primary HCC cells (Pnt-1/-2/-3/-4), or THLE-2 liver cells are cultured in WAY-600 (1-1000 nM)-containing medium for 24, 48, 72, 96 hours, cell viability is tested by MTT assay[2].
Animal AdminMice: Mice tumor xenografts are randomly divided into four groups (10 mice per group): vehicle ( intraperitoneal or i.p.), WAY-600 (10 mg/kg, i.p. injection), MEK-162 (2.5 mg/kg, oral gavage) or WAY-600 plus MEK-162 combination. The mice are monitored for activity and physical condition on daily basis, and mice body weights and tumor mass are measured weekly[2].
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.

[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.

Chemical & Physical Properties

Density1.4±0.1 g/cm3
Boiling Point678.1±55.0 °C at 760 mmHg
Molecular FormulaC28H30N8O
Molecular Weight494.591
Flash Point363.9±31.5 °C
Exact Mass494.254272
PSA87.99000
LogP1.30
Vapour Pressure0.0±2.1 mmHg at 25°C
Index of Refraction1.761
InChIKeyFPEIJQLXFHKLJV-UHFFFAOYSA-N
SMILESc1cncc(CN2CCC(n3ncc4c(N5CCOCC5)nc(-c5ccc6[nH]ccc6c5)nc43)CC2)c1
Storage condition-20℃

Synonyms

6-(1H-Indol-5-yl)-4-(4-morpholinyl)-1-[1-(3-pyridinylmethyl)-4-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidine
X7456
1H-Pyrazolo[3,4-d]pyrimidine, 6-(1H-indol-5-yl)-4-(4-morpholinyl)-1-[1-(3-pyridinylmethyl)-4-piperidinyl]-
WAY-600
pyrazolo pyrimidine,5u
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