AZ3246
Based on 1 Customer Validation
AZ3246 is an orally active and selective inhibitor of HPK1 with an IC50 of < 3 nM. AZ3246 induces IL-2 secretion in T cells with an EC50 of 90 nM. AZ3246 is a low-clearance antitumor compound that can be used for the study of breast cancer.
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 : 98.92%
- CAS 番号: 2893978-54-4
- 分子式: C21H20F3N9O
- 分子量:471.44
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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
- プロトコル
- 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
製品説明
体外実験
AZ3246 (100 nM) is highly selective for HPK1 over STK3, STK4, and TNIK , hits only HPK1 and MYLK at >80% inhibition, hits ROS1, YSK4 and TNIK at >50% inhibition[1].
AZ3246 has excellent metabolic stability in human liver microsomes[1].
AZ3246 induces IL-2 secretion in T cells with an EC50 of 90 nM without inhibiting antagonistic kinases[1].
AZ3246 exhibits low CLint values in primary human, rat, and dog hepatocytes. Low turnover was also observed in HμREL cocultures for rat, dog, monkey, and human hepatocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
AZ3246 (10-100 mg/kg; p.o.) exposure in mouse is linear up to 30 mg/kg with a limited increase in exposure at 100 mg/kg[1].
AZ3246 is a low-clearance compound, consistent with a neutral molecule that is not heavily metabolized by the liver[1].
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 mice with EMT6 cells injected subcutaneously into the right flank[1]
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Dosage:30 mg/kg
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Administration:Oral gavage (p.o.); twice daily
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Result:Inhibited tumor growth and similar to that of a monotherapy of 10 mg/kg murine anti-PD-L1 antibody (twice weekly)
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Animal Model:Female Balb/c mice with EMT6 cells injected subcutaneously into the right flank[1]
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Dosage:30 mg/kg
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Administration:Oral gavage (p.o.); twice daily
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Result:Inhibited tumor growth and similar to that of a monotherapy of 10 mg/kg murine anti-PD-L1 antibody (twice weekly).
化学情報
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CAS 番号 2893978-54-4
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性状 Solid
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分子量 471.44
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分子式 C21H20F3N9O
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Color Light yellow to yellow
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SMILES
FC(F)(CN1N=C(C)C(NC2=C(C(N)=O)N=C(C3=CN=CC4=C3N=CN4C)C(C5CC5)=N2)=C1)F
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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
体外:
DMSO : 50 mg/mL (106.06 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. 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 (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
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- 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 | 2.1212 mL | 10.6058 mL | 21.2116 mL | 53.0290 mL |
| 5 mM | 0.4242 mL | 2.1212 mL | 4.2423 mL | 10.6058 mL | |
| 10 mM | 0.2121 mL | 1.0606 mL | 2.1212 mL | 5.3029 mL | |
| 15 mM | 0.1414 mL | 0.7071 mL | 1.4141 mL | 3.5353 mL | |
| 20 mM | 0.1061 mL | 0.5303 mL | 1.0606 mL | 2.6515 mL | |
| 25 mM | 0.0848 mL | 0.4242 mL | 0.8485 mL | 2.1212 mL | |
| 30 mM | 0.0707 mL | 0.3535 mL | 0.7071 mL | 1.7676 mL | |
| 40 mM | 0.0530 mL | 0.2651 mL | 0.5303 mL | 1.3257 mL | |
| 50 mM | 0.0424 mL | 0.2121 mL | 0.4242 mL | 1.0606 mL | |
| 60 mM | 0.0354 mL | 0.1768 mL | 0.3535 mL | 0.8838 mL | |
| 80 mM | 0.0265 mL | 0.1326 mL | 0.2651 mL | 0.6629 mL | |
| 100 mM | 0.0212 mL | 0.1061 mL | 0.2121 mL | 0.5303 mL |
AZ3246 関連分類
HY-173006 関連分類
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