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Submit ReviewWYE 687 dihydrochloride is a 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.
Sold for research purposes under agreement from Pfizer Inc.
WYE 687 dihydrochloride is also offered as part of the Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
M. Wt | 601.53 |
Formula | C28H32N8O32HCl |
Storage | Desiccate at RT |
Purity | ≥98% (HPLC) |
CAS Number | 1702364-87-1 |
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
water | 60.15 | 100 | |
DMSO | 60.15 | 100 |
The following data is based on the product molecular weight 601.53. Batch specific molecular weights may vary from batch to batch due to the degree 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 |
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for WYE 687 dihydrochloride, please let us know.
Keywords: WYE 687 dihydrochloride, 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, Cell, Cycle, Inhibitors, 4282, Tocris Bioscience
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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