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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. 了解 Tocris 化合物库的更多信息。
分子量 | 601.53 |
公式 | C28H32N8O32HCl |
储存 | Desiccate at RT |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 60.15 | 100 | |
DMSO | 60.15 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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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关键词: 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
引用文献是使用了 Tocris 产品的出版物。 WYE 687 dihydrochloride 的部分引用包括:
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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This product guide reviews some of the main areas in cancer metabolism research and lists around 150 products that can be used to investigate metabolic pathways in cancer including:
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