HPK1-IN-2 dihydrochloride
Based on 1 Customer Validation
HPK1-IN-2 dihydrochloride is an orally active HPK1 inhibitor (IC50 < 0.05 µM) with antitumor activity. HPK1-IN-2 dihydrochloride 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.
- Purity: 98.03%
- CAS No.: 2375595-72-3
- Formula: C19H22Cl2N6OS
- Molecular Weight:453.39
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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) dihydrochloride 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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CAS No. 2375595-72-3
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Appearance Solid
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Molecular Weight 453.39
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Formula C19H22Cl2N6OS
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Color Light brown to brown
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SMILES
O=C1C(C2=NC3=CC=C(N4CCN(C)CC4)C=C3N2)=C(N)C(C=CS5)=C5N1.[H]Cl.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 100 mg/mL (220.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 25 mg/mL (55.14 mM; Need ultrasonic)
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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (275 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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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 (sealed storage, away from moisture and light). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.2056 mL | 11.0280 mL | 22.0561 mL | 55.1402 mL |
| 5 mM | 0.4411 mL | 2.2056 mL | 4.4112 mL | 11.0280 mL | |
| 10 mM | 0.2206 mL | 1.1028 mL | 2.2056 mL | 5.5140 mL | |
| 15 mM | 0.1470 mL | 0.7352 mL | 1.4704 mL | 3.6760 mL | |
| 20 mM | 0.1103 mL | 0.5514 mL | 1.1028 mL | 2.7570 mL | |
| 25 mM | 0.0882 mL | 0.4411 mL | 0.8822 mL | 2.2056 mL | |
| 30 mM | 0.0735 mL | 0.3676 mL | 0.7352 mL | 1.8380 mL | |
| 40 mM | 0.0551 mL | 0.2757 mL | 0.5514 mL | 1.3785 mL | |
| 50 mM | 0.0441 mL | 0.2206 mL | 0.4411 mL | 1.1028 mL | |
| DMSO | 60 mM | 0.0368 mL | 0.1838 mL | 0.3676 mL | 0.9190 mL |
| 80 mM | 0.0276 mL | 0.1379 mL | 0.2757 mL | 0.6893 mL | |
| 100 mM | 0.0221 mL | 0.1103 mL | 0.2206 mL | 0.5514 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.