HPK1-IN-2 TFA
Based on 1 Customer Validation
HPK1-IN-2 TFA is an orally active HPK1 inhibitor (IC50 <0.05 µM) with antitumor activity. HPK1-IN-2 TFA inhibits the activity of Lck (IC50 <0.05 µM) and Flt3 (IC50 < 0.05 µM) kinases.
For research use only. We do not sell to patients.
- Formula: C21H21F3N6O3S
- Molecular Weight:494.49
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All MAP4K Isoforms
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Biological Activity
IC50: <0.05 µΜ (HPK1); <0.05 µΜ (Flt3); 0.05-0.5 µΜ (Lck)[1]
HPK1-IN-2 (example A1) TFA suppresses SLP76 serine 376 phosphorylation and ERK1/2 T202/Y204 phosphorylation with IC50 values of 0.3-1 μM and > 3 μM, respectively, in α-CD3 stimulated Jurkat E6.1 cells[1].
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:Female BALB/c mice (6-8week old) injected with CT26 cancer cells[1]
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Dosage:75 mg/kg and 150 mg/kg
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Administration:Oral gavage; daily; for 21 days
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Result:Showed a dose-dependently tumor growth inhibition.
Chemical Information
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Molecular Weight 494.49
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Formula C21H21F3N6O3S
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SMILES
O=C1C(C2=NC3=CC=C(N4CCN(C)CC4)C=C3N2)=C(N)C(C=CS5)=C5N1.OC(C(F)(F)F)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
DMSO : 100 mg/mL (202.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0223 mL | 10.1114 mL | 20.2229 mL | 50.5571 mL |
| 5 mM | 0.4045 mL | 2.0223 mL | 4.0446 mL | 10.1114 mL | |
| 10 mM | 0.2022 mL | 1.0111 mL | 2.0223 mL | 5.0557 mL | |
| 15 mM | 0.1348 mL | 0.6741 mL | 1.3482 mL | 3.3705 mL | |
| 20 mM | 0.1011 mL | 0.5056 mL | 1.0111 mL | 2.5279 mL | |
| 25 mM | 0.0809 mL | 0.4045 mL | 0.8089 mL | 2.0223 mL | |
| 30 mM | 0.0674 mL | 0.3370 mL | 0.6741 mL | 1.6852 mL | |
| 40 mM | 0.0506 mL | 0.2528 mL | 0.5056 mL | 1.2639 mL | |
| 50 mM | 0.0404 mL | 0.2022 mL | 0.4045 mL | 1.0111 mL | |
| 60 mM | 0.0337 mL | 0.1685 mL | 0.3370 mL | 0.8426 mL | |
| 80 mM | 0.0253 mL | 0.1264 mL | 0.2528 mL | 0.6320 mL | |
| 100 mM | 0.0202 mL | 0.1011 mL | 0.2022 mL | 0.5056 mL |