HPK1-IN-3
Based on 1 Customer Validation
HPK1-IN-3 is a potent and selective ATP-competitive hematopoietic progenitor kinase 1 (HPK1; MAP4K1) inhibitor with an IC50 of 0.25 nM. HPK1-IN-3 has IL-2 cellular potency with an EC50 of 108 nM in human peripheral blood mononuclear cells (PBMCs).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.61%
- CAS. Nr.: 2739844-34-7
- Formel: C23H22F4N6O2
- Molecular Weight:490.45
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Speicherung: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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
HPK1 0.25 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| PBMC | EC50 |
108 nM
Compound: 27
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Antiinflammatory activity in human PBMC assessed as reduction in IL-2 production incubated for 16 to 18 hrs by ELISA
Antiinflammatory activity in human PBMC assessed as reduction in IL-2 production incubated for 16 to 18 hrs by ELISA
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[PMID: 33859804] |
In Vitro
HPK1-IN-3 (compound 27; 0.25-4 μM; 24-h) treatment shows a statistically significant elevation of proinflammatory cytokines IL-6 and TNF-α was observed in a concentration-dependent manner in human monocyte-derived dendritic cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS. Nr. 2739844-34-7
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Appearance Solid
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Molecular Weight 490.45
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Formel C23H22F4N6O2
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Color White to yellow
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SMILES
COC1=C(NC2=NC=C(C(N)=O)C(NC3=C(F)C=CC=C3C(F)(F)F)=N2)C=C4CN(C)CCC4=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 83.33 mg/mL (169.91 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. 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
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: ≥ 2.08 mg/mL (4.24 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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PBMC Thawing for Immune Assays
PBMC thawing for immune assays recovers viable cryopreserved peripheral blood mononuclear cells for downstream functional or phenotypic readouts, including ELISPOT, intracellular cytokine staining, proliferation assays, and flow-cytometric immunophenotyping. Cryopreserved PBMCs can support immune monitoring because antigen-specific T-cell function and major CD4/CD8 phenotypes may be retained after optimized freezing and thawing, although some lymphocyte subsets and activation or memory markers can be altered by cryopreservation. The technical objective is rapid warming of the frozen vial followed by controlled dilution and removal of DMSO-containing cryomedium, because thawing and wash conditions measurably affect viable PBMC recovery and downstream assay performance. Viability alone is insufficient for protocol evaluation because high viability may occur with low live-cell recovery, so both viable percentage and absolute live-cell recovery should be measured after thawing.
Reinheit & Dokumentation
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Data Sheet (277 KB)
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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)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
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 | 2.0389 mL | 10.1947 mL | 20.3894 mL | 50.9736 mL |
| 5 mM | 0.4078 mL | 2.0389 mL | 4.0779 mL | 10.1947 mL | |
| 10 mM | 0.2039 mL | 1.0195 mL | 2.0389 mL | 5.0974 mL | |
| 15 mM | 0.1359 mL | 0.6796 mL | 1.3593 mL | 3.3982 mL | |
| 20 mM | 0.1019 mL | 0.5097 mL | 1.0195 mL | 2.5487 mL | |
| 25 mM | 0.0816 mL | 0.4078 mL | 0.8156 mL | 2.0389 mL | |
| 30 mM | 0.0680 mL | 0.3398 mL | 0.6796 mL | 1.6991 mL | |
| 40 mM | 0.0510 mL | 0.2549 mL | 0.5097 mL | 1.2743 mL | |
| 50 mM | 0.0408 mL | 0.2039 mL | 0.4078 mL | 1.0195 mL | |
| 60 mM | 0.0340 mL | 0.1699 mL | 0.3398 mL | 0.8496 mL | |
| 80 mM | 0.0255 mL | 0.1274 mL | 0.2549 mL | 0.6372 mL | |
| 100 mM | 0.0204 mL | 0.1019 mL | 0.2039 mL | 0.5097 mL |
HPK1-IN-3 Related Classifications
HY-138568 Related Classifications
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