WYE 687 dihydrochloride

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Cat.No. 4282 - WYE 687 dihydrochloride | C28H32N8O3 | CAS No. 1062161-90-3
Description: Potent and selective mTOR inhibitor
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
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Literature
Pathways

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.

Compound Libraries

WYE 687 dihydrochloride is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 601.53
Formula C28H32N8O3
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 1062161-90-3
PubChem ID 90488926
InChI Key ZQJPHAXLAKKXIX-UHFFFAOYSA-N
Smiles O=C(OC)NC(C=C4)=CC=C4C1=NC(N3CCOCC3)=C2C(N(C5CCN(CC6=CN=CC=C6)CC5)N=C2)=N1.Cl.Cl

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 60.15 100
water 60.15 100

Preparing Stock Solutions

The following data is based on the product molecular weight 601.53. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.66 mL 8.31 mL 16.62 mL
5 mM 0.33 mL 1.66 mL 3.32 mL
10 mM 0.17 mL 0.83 mL 1.66 mL
50 mM 0.03 mL 0.17 mL 0.33 mL

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Product Datasheets

Safety Datasheet

References

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 6232 PMID: 19584280


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View Related Products by Product Action

View all mTOR Inhibitors

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, mTOR, Cell, Cycle, Inhibitors, mTOR, Tocris Bioscience

1 Citation for WYE 687 dihydrochloride

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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Literature in this Area

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Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Pain

Pain Research Product Guide

A collection of over 250 products for pain research, the guide includes research tools for the study of:

  • Nociception
  • Ion Channels
  • G-Protein-Coupled Receptors
  • Intracellular Signaling

Pathways for WYE 687 dihydrochloride

mTOR

mTOR Signaling Pathway

mTOR is a serine/threonine kinase that nucleates at multiprotein complexes mTORC1 and mTORC2. Signaling by these complexes regulates cell growth, proliferation and survival.