WYE 687 dihydrochloride

Cat. No. 4282

WYE 687 dihydrochloride C28H32N8O3 [1062161-90-3]

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Chemical Name: N-[4-[4-(4-Morpholinyl)-1-[1-(3-pyridinylmethyl)-4-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-carbamic acid methyl ester hydrochloride

Biological Activity

Potent, ATP-competitive inhibitor of mammalian target of rapamycin (mTOR) (IC50 = 7 nM). Displays selectivity for mTOR over PI 3-Kα (~100-fold) and PI 3-Kγ (~500-fold). Inhibits phosphorylation of mTORC1 and mTORC2 substrates including S6K, SGK and Akt; blocks VEGF secretion and HIF-1α expression. Exhibits antiproliferative effects in cancer cell lines through G1 cell cycle arrest and selective apoptosis.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M.Wt:
601.53
Formula:
C28H32N8O3
Solubility:
Soluble to 100 mM in water and to 100 mM in DMSO
Purity:
>98 %
Storage:
Desiccate at RT
CAS No:
1062161-90-3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Yu et al (2009) Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin. Cancer.Res. 69 (15) 6232. PMID: 19584280.

If you know of a relevant reference for WYE 687 dihydrochloride please let us know.

Citations are publications that use Tocris products. Selected citations for WYE 687 dihydrochloride include:

Saric et al (2016) mTOR controls lysosome tubulation and antigen presentation in macrophages and dendritic cells. Data Brief 27 321. PMID: 26582390.

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View Related Products by Product Action

Keywords: WYE 687 dihydrochloride, supplier, mTOR, WYE687, mammalian, target, rapamycin, inhibitors, inhibits, ATP, competitive, potent, selective, antiproliferatives, mTORC1, mTORC2, S6K, SGk, Akt, blocks, VEGF, secretion, HIF-1alpha, HIF-1a, antiproliferative, cell, cycle, arrest, apoptosis, Tocris Bioscience, mTOR Inhibitor products

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