THRX-144644
Based on 1 Customer Validation
THRX-144644 is a Lung-restricted ALK5 inhibitor with an IC50 value of 0.14 nM. THRX-144644 avoids systemic toxicities associated with TGFβ pathway inhibition.
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: 99.43%
- CAS 番号: 2442519-59-5
- 分子式: C26H28ClF2N7
- 分子量:512.00
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保管条件:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
生物活性
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ALK5 0.14 nM (IC50) |
THRX-144644 (1-10000 nM; 1 h) inhibits ALK5 with an IC50 value of 23 nM in human BEAS2B cell line.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague Dawley rats[1]
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Dosage:2, 10, and 60 mg/kg
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Administration:Inhalation: nebulizer, daily, for 14 days
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Result:Had the L:P ratio (AUC) was 0.44.
Had lung-to-plasma ratios ranged from 100- to 1200-fold in rats across dose level.
Had lung trough (24 h) concentrations in rats ranged from 3- to 17-fold above the PCLS IC50 across tolerated doses.
化学情報
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CAS 番号 2442519-59-5
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性状 Solid
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分子量 512.00
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分子式 C26H28ClF2N7
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Color White to yellow
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SMILES
FC1=CC(F)=C(C2=NNC=C2C3=NC4=C(C=C3)N=CC(NCCN5CCN(C(C)C)CC5)=C4)C=C1Cl
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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, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶剤 & 溶解度
DMSO : 50 mg/mL (97.66 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 (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). 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 (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 (protect from light, stored under nitrogen). 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 | 1.9531 mL | 9.7656 mL | 19.5312 mL | 48.8281 mL |
| 5 mM | 0.3906 mL | 1.9531 mL | 3.9062 mL | 9.7656 mL | |
| 10 mM | 0.1953 mL | 0.9766 mL | 1.9531 mL | 4.8828 mL | |
| 15 mM | 0.1302 mL | 0.6510 mL | 1.3021 mL | 3.2552 mL | |
| 20 mM | 0.0977 mL | 0.4883 mL | 0.9766 mL | 2.4414 mL | |
| 25 mM | 0.0781 mL | 0.3906 mL | 0.7812 mL | 1.9531 mL | |
| 30 mM | 0.0651 mL | 0.3255 mL | 0.6510 mL | 1.6276 mL | |
| 40 mM | 0.0488 mL | 0.2441 mL | 0.4883 mL | 1.2207 mL | |
| 50 mM | 0.0391 mL | 0.1953 mL | 0.3906 mL | 0.9766 mL | |
| 60 mM | 0.0326 mL | 0.1628 mL | 0.3255 mL | 0.8138 mL | |
| 80 mM | 0.0244 mL | 0.1221 mL | 0.2441 mL | 0.6104 mL |