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WAY-600

WAY-600

产品编号 T6730   CAS 1062159-35-6
别名: 6-(1H-吲哚-5-基)-4-(4-吗啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶, WAY600

WAY-600 是一种有效的,选择性的,ATP 竞争型的mTOR 抑制剂,抑制重组 mTOR 酶,其 IC50=9 nM。它能够阻断 mTOR 复合物 1/2 (mTORC1/2) 组装和激活。

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WAY-600 Chemical Structure
WAY-600, CAS 1062159-35-6
规格 价格/CNY 货期 数量
1 mg ¥ 522 现货
2 mg ¥ 913 现货
5 mg ¥ 1,580 现货
10 mg ¥ 2,160 现货
25 mg ¥ 3,780 现货
50 mg ¥ 5,420 现货
100 mg ¥ 7,620 现货
500 mg ¥ 15,200 现货
1 mL * 10 mM (in DMSO) ¥ 1,690 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
Doxorubicin hydrochloride限时半价
产品目录号及名称: WAY-600 (T6730)
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纯度: 99.63%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 WAY-600 is a potent, ATP-competitive and selective inhibitor of mTOR with IC50 of 9 nM; blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) but not P-AKT(T308); selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
靶点活性 mTOR:9 nM
体外活性 Immune-complex kinase assay shows mTORC2-specific substrate His6-AKT or the mTORC1 substrate His6-S6K is dose dependently inhibited by WAY-600. WAY-600 globally inhibits mTOR signaling and AKT function in cellular models dose dependently. WAY-600 profoundly inhibits cap-dependent and global protein synthesis in MDA361, human breast cancer cells. WAY-600 shows antiproliferative effects in various cancer cell lines involving G1 cell cycle arrest and selective apoptosis. WAY-600 down-regulate angiogenic factors, VEGF and HIF-1α, in U87 mg, MDA361 and LNCap cells. [1]
激酶实验 DELFIA Format of Purified FLAG-TOR: The routine assays with purified FLAG-TOR (FL and 3.5) are performed in 96-well plates as follows. Enzymes are first diluted in kinase assay buffer (10 mM Hepes (pH 7.4), 50 mM NaCl, 50 mM β-glycerophosphate, 10 mM MnCl2, 0.5 mM DTT, 0.25 lM microcystin LR, and 100 lg/mL BSA). To each well, 12 μL of the diluted enzyme is mixed briefly with 0.5 μL test inhibitor or control vehicle dimethyl sulfoxide (DMSO). The kinase reaction is initiated by adding 12.5 μL kinase assay buffer containing ATP and His6-S6K to give a final reaction volume of 25 μL containing 800 ng/mL FLAG-TOR, 100 μM ATP, and 1.25 μM His6-S6K. The reaction plate is incubated for 2 hours (linear at 1–6 hour) at room temperature with gentle shaking and then terminated by adding 25 μL Stop buffer (20 mM Hepes (pH 7.4), 20 mM EDTA, and 20 mM EGTA). The DELFIA detection of the phosphorylated (Thr-389) His6-S6K is performed at room temperature using a monoclonal anti-P(T389)- p70S6K antibody (1A5) labeled with Europium-N1- ITC (Eu) (10.4 Eu per antibody). Fortyfive microliters of the terminated kinase reaction mixture are transferred to a MaxiSorp plate containing 55 μL PBS. The His6-S6K is allowed to attach for 2 hour after which the wells are aspirated and washed once with PBS. One hundred microliters of DELFIA buffer with 40 ng/mL Eu-P(T389)-S6K antibody is added. The antibody binding is continued for 1 hour with gentle agitation. The wells are then aspirated and washed four times with PBS containing 0.05% Tween 20 (PBST). One hundred microliters of DELFIA Enhancement solution is added to each well and the plates are read in a PerkinElmer Victor model plate reader. Data obtained are used to calculate enzymatic activity and enzyme inhibition by potential inhibitors.
细胞实验 For cell cycle analysis, cells are seeded in 96-well culture plates at 10,000 cells per well for 24 hours, treated with various inhibitors for 24 hours or 48 hours. Following treatment, cells are harvested, washed with PBS and fixed overnight at -20 °C in 70% ethanol. Cells are washed, stained with propidium iodide and analyzed for cell cycle profile (acquired 5000 cells/well) on Guava PCA-96 instrument according to the Guava Cell Cycle Protocol(Only for Reference)
别名 6-(1H-吲哚-5-基)-4-(4-吗啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶, WAY600
分子量 494.59
分子式 C28H30N8O
CAS No. 1062159-35-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 2 mg/mL (4.04 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 22 mg/mL (44.48 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.0219 mL 10.1094 mL 20.2188 mL 50.5469 mL
DMSO 5 mM 0.4044 mL 2.0219 mL 4.0438 mL 10.1094 mL
10 mM 0.2022 mL 1.0109 mL 2.0219 mL 5.0547 mL
20 mM 0.1011 mL 0.5055 mL 1.0109 mL 2.5273 mL

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TargetMol Library Books参考文献

1. Yu K, et al, Cancer Res, 2009, 69(15), 6232-6240.
SU 4981 Ranibizumab Pazopanib Hydrochloride Pz-1 Chiauranib WHI-P180 Treprostinil Sodium Regorafenib monohydrate

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 高选择性抑制剂库 酪氨酸激酶分子库 激酶抑制剂库 膜蛋白靶向化合物库 血管生成库 抗氧化化合物库 已知活性化合物库 免疫/炎症分子化合物库 抗衰老化合物库

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体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

WAY-600 1062159-35-6 Angiogenesis PI3K/Akt/mTOR signaling Tyrosine Kinase/Adaptors VEGFR PI3K Src mTOR WAY 600 inhibit 6-(1H-吲哚-5-基)-4-(4-吗啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶 WAY600 Inhibitor Mammalian target of Rapamycin inhibitor

 

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