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.
For research use only. We do not sell to patients.
- Purity: 98.92%
- CAS No.: 2893978-54-4
- Formula: C21H20F3N9O
- Molecular Weight:471.44
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Immunology/Inflammation Compound Library
HY-L007
-
Kinase Inhibitor Library
HY-L009
-
MAPK Compound Library
HY-L010
-
Anti-Cancer Compound Library
HY-L025
-
Clinical Compound Library
HY-L026
-
Oxygen Sensing Compound Library
HY-L045
-
Orally Active Compound Library
HY-L061
-
Anti-Breast Cancer Compound Library
HY-L074
-
Anti-Lung Cancer Compound Library
HY-L075
-
Anti-Obesity Compound Library
HY-L087
-
Angiogenesis-Related Compound Library
HY-L088
-
Highly Selective Inhibitors Library
HY-L158
-
Highly Selective Activators Library
HY-L159
-
Serine/Threonine Kinase Inhibitor Library
HY-L164
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
High-Throughput Bioactive Compound Library
HY-L205
All MAP4K Isoforms
More
Biological Activity
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.
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.
-
Animal Model:Female Balb/c mice with EMT6 cells injected subcutaneously into the right flank[1]
-
Dosage:30 mg/kg
-
Administration:Oral gavage (p.o.); twice daily
-
Result:Inhibited tumor growth and similar to that of a monotherapy of 10 mg/kg murine anti-PD-L1 antibody (twice weekly)
-
Animal Model:Female Balb/c mice with EMT6 cells injected subcutaneously into the right flank[1]
-
Dosage:30 mg/kg
-
Administration:Oral gavage (p.o.); twice daily
-
Result:Inhibited tumor growth and similar to that of a monotherapy of 10 mg/kg murine anti-PD-L1 antibody (twice weekly).
Chemical Information
-
CAS No. 2893978-54-4
-
Appearance Solid
-
Molecular Weight 471.44
-
Formula C21H20F3N9O
-
Color Light yellow to yellow
-
SMILES
FC(F)(CN1N=C(C)C(NC2=C(C(N)=O)N=C(C3=CN=CC4=C3N=CN4C)C(C5CC5)=N2)=C1)F
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
-
Data Sheet (278 KB)
-
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)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
References
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 |
Powered by Bioz