WRX606
Based on 1 Customer Validation
WRX606 is an orally active nonrapalog inhibitor for mTOR complex 1 (mTORC1M). WRX606 inhibits the phosphorylation of mTORC1 substrate S6 kinase 1 (S6K1) (IC50 = 10 nM) and eukaryotic translation initiation factor 4E binding protein (p-4E-BP1) (IC50 = 0.27 μM) in MCF-7 cells. WRX606 suppresses tumor growth in mice without promotion of metastasis. WRX606 can be studied in research as an antitumor agent.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 95.65%
- CAS 番号: 899937-47-4
- 分子式: C28H25ClN4O6
- 分子量:548.97
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
生物活性
WRX606 (1 μM) induces ternary complex formation in HEK293 cells[1].
WRX606 (100 nM-100 M, 72 h) inhibits cancer cell (HeLa and MCF-7) growth via cytotoxic effects[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa and MCF-7
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Concentration:100 nM, 10 μM, 100 mM, 10 M, 100 M
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Incubation Time:72 h
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Result:Resulted in a decrease in the cell viability of both HeLa (IC50 = 3.5 nM) and MCF-7 (IC50 = 62.3 nM) cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c cancer-bearing mice with 4T1 breast cancer cells orthotopically implanted into the mammary fat pad[1]
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Dosage:25 mg/kg/day
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Administration:Oral gavage (p.o.) for 10 days
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Result:Significantly suppressed tumor growth compared to the controls.
Did not promote tumor metastasis.
Had no adverse effects in kidney and liver functions.
化学情報
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CAS 番号 899937-47-4
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性状 Solid
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分子量 548.97
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分子式 C28H25ClN4O6
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Color White to off-white
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SMILES
O=C(CN1C(N(CCCC(NCC2=CC=C3OCOC3=C2)=O)C(C4=C1C=CC=C4)=O)=O)NC5=CC(Cl)=CC=C5
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
DMSO : 25 mg/mL (45.54 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Shams R, et al., In Silico and In Cell Hybrid Selection of Nonrapalog Ligands to Allosterically Inhibit the Kinase Activity of mTORC1. J Med Chem. 2022 Jan 27;65(2):1329-1341. [Content Brief]
[2]. Li, S., et al., (2023). MNK, mTOR or eIF4E-selecting the best anti-tumor target for blocking translation initiation. European journal of medicinal chemistry, 260, 115781. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8216 mL | 9.1080 mL | 18.2159 mL | 45.5398 mL |
| 5 mM | 0.3643 mL | 1.8216 mL | 3.6432 mL | 9.1080 mL | |
| 10 mM | 0.1822 mL | 0.9108 mL | 1.8216 mL | 4.5540 mL | |
| 15 mM | 0.1214 mL | 0.6072 mL | 1.2144 mL | 3.0360 mL | |
| 20 mM | 0.0911 mL | 0.4554 mL | 0.9108 mL | 2.2770 mL | |
| 25 mM | 0.0729 mL | 0.3643 mL | 0.7286 mL | 1.8216 mL | |
| 30 mM | 0.0607 mL | 0.3036 mL | 0.6072 mL | 1.5180 mL | |
| 40 mM | 0.0455 mL | 0.2277 mL | 0.4554 mL | 1.1385 mL |