ART5537
Based on 1 Customer Validation
EXO1 inhibitor, LLE, FEN1, Olaparib, breast cancer, Colorectal Adenocarcinoma
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: 99.84%
- 分子式: C23H18ClN5O3
- 分子量:447.87
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
ART5537 (0.0001-10 μM) displays unambiguous dose-dependent cellular target engagement with an EC50 = 55 nM[1].
ART5537 (0.001-10 μM) has no activation HAP1 EXO1 KO cells, shows no further effect over KO of EXO1 (∼ 50% reduction) and induces a dose-dependent retention of GPF2-EXO1 on chromatin in a U-2 OS Flp-In line [1].
ART5537 (7 days) is not a broadly cytotoxic and has a mild EXO1-dependent sensitivity in MDA-MB-436 (EC50 = 4.0 nM), HCC 1937 (EC50 = 5.3 nM), SUM 149PT (EC50 = 5.0 nM) and HCC38 (EC50 = 8.3 nM) cells[1].
ART5537 (5 days) exhibits no ubiquitous cytotoxicity in HCT116 cells following cotreatment with Olaparib (HY-10162) [1].
ART5537 (7 days) combined with Olaparib exerts a strong synergistic effect in radiation-treated wild-type HCT116 cells, but no such effect is observed in the two radiation-treated EXO1 knockout clones[1].
ART5537 (0.01-100 μM, 6 days) effectively inhibits EXO1, and when combined with Olaparib in radiation-treated HCT116 cells, it significantly enhances the cancer cell-killing effect and greatly increases the activity potency[1].
ART5537 inhibits EXO1 in HCT116 cells and results in a > 40-fold sensitization, has suitable physicochemical properties for use as a cell probe with high thermodynamic solubility and good passive permeability and is unstable in human and mouse liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 cells
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Concentration:0.01, 0.1, 10 and 100 μM
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Incubation Time:6 days
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Result:Resulted a > 40-fold sensitization.
Potently sensitized cells irradiated with 3 × 1 Gy (EC50 = 144 nM).
| Species | Dose | Route | CL_obs | T1/2 | Vss |
|---|---|---|---|---|---|
| Mice[1] | 0.2 mg/kg | i.v. | 111 mL/min/kg | 0.7 h | 5.7 L/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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性状 Solid
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分子量 447.87
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分子式 C23H18ClN5O3
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Color White to off-white
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SMILES
C[C@@H](C1=CC=CC=C1)N2CN(C3=NC=C(Cl)C4=C3C=NC=C4)N5C=CC(C(O)=C5C2=O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 50 mg/mL (111.64 mM; Need ultrasonic; 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. 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. 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 (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
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. 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 | 2.2328 mL | 11.1640 mL | 22.3279 mL | 55.8198 mL |
| 5 mM | 0.4466 mL | 2.2328 mL | 4.4656 mL | 11.1640 mL | |
| 10 mM | 0.2233 mL | 1.1164 mL | 2.2328 mL | 5.5820 mL | |
| 15 mM | 0.1489 mL | 0.7443 mL | 1.4885 mL | 3.7213 mL | |
| 20 mM | 0.1116 mL | 0.5582 mL | 1.1164 mL | 2.7910 mL | |
| 25 mM | 0.0893 mL | 0.4466 mL | 0.8931 mL | 2.2328 mL | |
| 30 mM | 0.0744 mL | 0.3721 mL | 0.7443 mL | 1.8607 mL | |
| 40 mM | 0.0558 mL | 0.2791 mL | 0.5582 mL | 1.3955 mL | |
| 50 mM | 0.0447 mL | 0.2233 mL | 0.4466 mL | 1.1164 mL | |
| 60 mM | 0.0372 mL | 0.1861 mL | 0.3721 mL | 0.9303 mL | |
| 80 mM | 0.0279 mL | 0.1395 mL | 0.2791 mL | 0.6977 mL | |
| 100 mM | 0.0223 mL | 0.1116 mL | 0.2233 mL | 0.5582 mL |
ART5537 関連分類
HY-180573 関連分類
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