DI-82
Based on 1 Customer Validation
DI-82 is a potent deoxycytidine kinase (dCK) inhibitor with an IC50app of 27.8 nM and Kiapp of 9.2 nM. DI-82 has antitumor activity.
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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: 98.0%
- CAS 番号: 1638148-50-1
- 分子式: C20H26N6O4S3
- 分子量:510.65
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保管条件:Powder -20°C, 3 years , 4°C, 2 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
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CCRF-CEM | IC50 |
3.7 nM
Compound: 12R
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Inhibition of dCK in human CCRF-CEM cells assessed as inhibition of [3H]-dC uptake by scintillation counting analysis
Inhibition of dCK in human CCRF-CEM cells assessed as inhibition of [3H]-dC uptake by scintillation counting analysis
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[PMID: 25341194] |
DI-82 (compound 12R) has an IC50 of 3.7 nM in CCRF-CEM acute lymphoblastic leukemia cells[1].
DI-82 (1 μM) has a NADPH-dependent CLint of 22.7 μL/min?mg and a NADPH-dependent T1/2 of 102 mins in a standard microsomal liver clearance assay[1].
DI-82 (200?μM) completely blunts the ability of decitabine to bind human thymidylate synthase (TS)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1638148-50-1
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性状 Solid
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分子量 510.65
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分子式 C20H26N6O4S3
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Color White to light yellow
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SMILES
NC1=NC(S[C@H](C)C(N=C2C(C=C3OCCNS(=O)(C)=O)=CC=C3OC)=C(S2)C)=NC(N)=C1
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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 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 120 mg/mL (234.99 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 (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Julian Nomme, et al. Structure-guided Development of Deoxycytidine Kinase Inhibitors With Nanomolar Affinity and Improved Metabolic Stability. J Med Chem. 2014 Nov 26;57(22):9480-94. [Content Brief]
[2]. Helena Almqvist, et al. CETSA Screening Identifies Known and Novel Thymidylate Synthase Inhibitors and Slow Intracellular Activation of 5-fluorouracil. Nat Commun. 2016 Mar 24;7:11040. [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. 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 | 1.9583 mL | 9.7914 mL | 19.5829 mL | 48.9572 mL |
| 5 mM | 0.3917 mL | 1.9583 mL | 3.9166 mL | 9.7914 mL | |
| 10 mM | 0.1958 mL | 0.9791 mL | 1.9583 mL | 4.8957 mL | |
| 15 mM | 0.1306 mL | 0.6528 mL | 1.3055 mL | 3.2638 mL | |
| 20 mM | 0.0979 mL | 0.4896 mL | 0.9791 mL | 2.4479 mL | |
| 25 mM | 0.0783 mL | 0.3917 mL | 0.7833 mL | 1.9583 mL | |
| 30 mM | 0.0653 mL | 0.3264 mL | 0.6528 mL | 1.6319 mL | |
| 40 mM | 0.0490 mL | 0.2448 mL | 0.4896 mL | 1.2239 mL | |
| 50 mM | 0.0392 mL | 0.1958 mL | 0.3917 mL | 0.9791 mL | |
| 60 mM | 0.0326 mL | 0.1632 mL | 0.3264 mL | 0.8160 mL | |
| 80 mM | 0.0245 mL | 0.1224 mL | 0.2448 mL | 0.6120 mL | |
| 100 mM | 0.0196 mL | 0.0979 mL | 0.1958 mL | 0.4896 mL |
DI-82 関連分類
HY-136499 関連分類
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