| Size | Price | Stock | Qty |
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| 25mg |
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Purity: ≥98%
WAY-600 (WAY600) is a novel, potent, ATP-competitive and selective inhibitor of mTOR (mammalian target of rapamycin) with potential antitumor activity. It exhibits strong antiproliferative activity in a number of cancer cell lines and high antitumor efficacy in vivo. It inhibits mTOR with an IC50 of 9 nM.
| Targets |
mTOR (IC50 = 9 nM); PI3K alpha (IC50 = 1.96 μM); PI3K gamma (IC50 = 8.45 μM); mTORC1; mTORC2
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| ln Vitro |
WAY-600 exhibits a concentration-dependent and time-dependent inhibition of f HepG2 and Huh-7 cells viability. The number of HepG2 cell colonies is significantly reduced after treatment with WAY-600 (1-1000 nM). Meanwhile, treatment with WAY-600 also prevents BrdU incorporation in HepG2 cells. In HepG2 cells, WAY-600 dose-dependently raises caspase-3 and caspase-9 activity. mTORC1 (mTOR-Raptor association) and mTORC2 (mTOR-Rictor association) assembly is disrupted by WAY-600. WAY-600 (100 nM) almost completely inhibits the activation of mTORC1 (indicated by p-S6K1 and p-4E-BP1) and mTORC2[2].
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| ln Vivo |
Way-600 (10 mg/kg, daily) treatment prevents HepG2 tumor development in naked mice. The daily HepG2 tumor growth in mice receiving WAY-600 is significantly slower than in mice receiving vehicle control. Importantly, the co-administration of MEK-162 (2.5 mg/kg, p.o. daily) enhances the in vivo anti-cancer activity of WAY-600[2].
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| Enzyme Assay |
In 96-well plates, the following routine assays are run using purified FLAG-TOR (FL and 3.5). Initially, the enzymes are 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). Dimethyl sulfoxide (DMSO), a control substance, and 12 L of the diluted enzyme are briefly combined in each well. The kinase reaction is started by adding 12.5 μL of kinase assay buffer containing ATP and His6-S6K to create a final reaction volume of 25 L that contains 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 hours) at room temperature with gentle shaking before being stopped by adding 25 L of stop buffer (20 mM Hepes (pH 7.4), 20 mM EDTA, and 20 mM EGTA). Using a monoclonal anti-P(T389)-p70S6K antibody (1A5) labeled with Europium-N1-ITC (Eu) (10.4 Eu per antibody), the phosphorylated (Thr-389) His6-S6K is detected by DELFIA at room temperature.
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| Cell Assay |
Cells are seeded in 96-well culture plates at a density of 10,000 cells per well for 24 hours before being exposed to different inhibitors for 24 or 48 hours. Following treatment, cells are collected, cleaned with PBS, and fixed for an overnight period at -20 °C in 70% ethanol. In accordance with the Guava Cell Cycle Protocol, cells are washed, stained with propidium iodide, and examined for cell cycle profile (acquired 5000 cells/well).
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| Animal Protocol |
Mice: WAY-600 (10 mg/kg, intraperitoneal injection), MEK-162 (2.5 mg/kg, oral gavage), WAY-600 plus MEK-162 combination, and vehicle (10 mice per group) are administered to mice with tumor xenografts. The mice's daily activity and physical condition are observed, and their body weights and tumor masses are measured every week[2].
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| References |
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| Molecular Formula |
C28H30N8O
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|---|---|
| Molecular Weight |
494.590804576874
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| Exact Mass |
494.25426
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| Elemental Analysis |
C, 68.00; H, 6.11; N, 22.66; O, 3.23
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| CAS # |
1062159-35-6
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| Related CAS # |
1062159-35-6
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| Appearance |
White solid powder
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| SMILES |
C1CN(CCC1N2C3=C(C=N2)C(=NC(=N3)C4=CC5=C(C=C4)NC=C5)N6CCOCC6)CC7=CN=CC=C7
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| InChi Key |
FPEIJQLXFHKLJV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H30N8O/c1-2-20(17-29-8-1)19-34-10-6-23(7-11-34)36-28-24(18-31-36)27(35-12-14-37-15-13-35)32-26(33-28)22-3-4-25-21(16-22)5-9-30-25/h1-5,8-9,16-18,23,30H,6-7,10-15,19H2
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| Chemical Name |
4-(6-(1H-indol-5-yl)-1-(1-(pyridin-3-ylmethyl)piperidin-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)morpholine
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| Synonyms |
WAY600; WAY600;WAY 600
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~22 mg/mL (~44.5 mM)
Water: <1 mg/mL Ethanol: ~20 mg/mL (~46.6 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.05 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0219 mL | 10.1094 mL | 20.2188 mL | |
| 5 mM | 0.4044 mL | 2.0219 mL | 4.0438 mL | |
| 10 mM | 0.2022 mL | 1.0109 mL | 2.0219 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Cancer Res. 2009 Aug 1;69(15):6232-40 |
Cancer Res. 2009 Aug 1;69(15):6232-40 |
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