GSK973
Based on 1 Customer Validation
GSK973, a chemical probe, is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5).
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 : 99.97%
- CAS 番号: 2138473-38-6
- 分子式: C23H23FN2O4
- 分子量:410.44
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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
製品説明
IC50 & Target
[1]|
BRD4 BD2 7.8 (pIC50) |
BRD2 BD2 7.5 (pIC50) |
BRD3 BD2 7.8 (pIC50) |
BRDT BD2 7.4 (pIC50) |
BRD4 BD2 8.7 (pKd) |
BRD2 BD2 8.3 (pKd) |
BRD3 BD2 8.5 (pKd) |
BRDT BD2 8.3 (pKd) |
体内実験
GSK973 (3 mg/kg; p.o) treatment shows the Fpo of 48%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar Han Rats[1]
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Dosage:1 mg/kg (Pharmacokinetic Analysis)
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Administration:I.v.
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Result:The CL, CIrenal, Vss, and T1/2 were 73 mL/min/kg, 4 mL/min/kg, 2.1L/kg, and 0.6 hours, respectively.
化学情報
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CAS 番号 2138473-38-6
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性状 Solid
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分子量 410.44
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分子式 C23H23FN2O4
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Color Off-white to light yellow
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SMILES
[H][C@]1([C@@H]2NC(C3=CC(C(NC)=O)=C4C([C@@H]([C@H](O4)CF)C5=CC=CC=C5)=C3)=O)[C@]2([H])COC1
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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
体外:
DMSO : 125 mg/mL (304.55 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 (277 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
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 | 2.4364 mL | 12.1820 mL | 24.3641 mL | 60.9102 mL |
| 5 mM | 0.4873 mL | 2.4364 mL | 4.8728 mL | 12.1820 mL | |
| 10 mM | 0.2436 mL | 1.2182 mL | 2.4364 mL | 6.0910 mL | |
| 15 mM | 0.1624 mL | 0.8121 mL | 1.6243 mL | 4.0607 mL | |
| 20 mM | 0.1218 mL | 0.6091 mL | 1.2182 mL | 3.0455 mL | |
| 25 mM | 0.0975 mL | 0.4873 mL | 0.9746 mL | 2.4364 mL | |
| 30 mM | 0.0812 mL | 0.4061 mL | 0.8121 mL | 2.0303 mL | |
| 40 mM | 0.0609 mL | 0.3046 mL | 0.6091 mL | 1.5228 mL | |
| 50 mM | 0.0487 mL | 0.2436 mL | 0.4873 mL | 1.2182 mL | |
| 60 mM | 0.0406 mL | 0.2030 mL | 0.4061 mL | 1.0152 mL | |
| 80 mM | 0.0305 mL | 0.1523 mL | 0.3046 mL | 0.7614 mL | |
| 100 mM | 0.0244 mL | 0.1218 mL | 0.2436 mL | 0.6091 mL |
GSK973 関連分類
HY-138563 関連分類
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