HPK1-IN-7
Based on 1 Customer Validation
HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1.
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- Pureté : 99.11%
- CAS No.: 2320462-65-3
- Formule: C24H22N6O4
- Masse moléculaire:458.47
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
HPK1 2.6 nM (IC50) |
GLK/MAP4K3 140 nM (IC50) |
IRAK4 59 nM (IC50) |
Fms/CSFR 3.2 nM (IC50) |
FLT3 25.4 nM (IC50) |
AMPKA1 44.3 nM (IC50) |
cKIT 45.7 nM (IC50) |
MST1 55.1 nM (IC50) |
ICK 65.1 nM (IC50) |
MST2 78.5 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| T-cell | IC50 |
>5000 nM
Compound: 4
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Cytotoxicity against Balb/c mouse derived anti-CD28-stimulated Pan T cells assessed as reduction in cell viability by Cell Titer Glo assay
Cytotoxicity against Balb/c mouse derived anti-CD28-stimulated Pan T cells assessed as reduction in cell viability by Cell Titer Glo assay
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[PMID: 36542759] |
In Vivo
HPK1-IN-7 (compound 24) (1 mg/kg; intravenous; mice) is characterized by moderate plasma clearance (43 mL/min/kg) and a large volume of distribution (4.4 L/kg). After oral administration (20 mg/kg), the Cmax was 5.3 μM and the AUC0-24h was 19 μM h. The calculated oral bioavailability based on these pharmacokinetics studies is approximately 100%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice (MC38 syngeneic tumor model)[1]
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Dosage:100 mg/kg
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Administration:Oral; twice daily for 28 days
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Result:Enhanced the efficacy of anti-PD1 treatment, garnering a 100% cure rate vs a 20% cure rate with anti-PD1 alone.
Chemical Information
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CAS No. 2320462-65-3
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Appearance Solid
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Masse moléculaire 458.47
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Formule C24H22N6O4
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Color White to off-white
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SMILES
O=C1OC(C)(C)C2=C1C=CC(NC3=NC=C(C4=NN=CO4)C(N[C@@H](C5=CC=CC=C5)CO)=N3)=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 125 mg/mL (272.65 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (4.54 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.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
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 | 2.1812 mL | 10.9058 mL | 21.8117 mL | 54.5292 mL |
| 5 mM | 0.4362 mL | 2.1812 mL | 4.3623 mL | 10.9058 mL | |
| 10 mM | 0.2181 mL | 1.0906 mL | 2.1812 mL | 5.4529 mL | |
| 15 mM | 0.1454 mL | 0.7271 mL | 1.4541 mL | 3.6353 mL | |
| 20 mM | 0.1091 mL | 0.5453 mL | 1.0906 mL | 2.7265 mL | |
| 25 mM | 0.0872 mL | 0.4362 mL | 0.8725 mL | 2.1812 mL | |
| 30 mM | 0.0727 mL | 0.3635 mL | 0.7271 mL | 1.8176 mL | |
| 40 mM | 0.0545 mL | 0.2726 mL | 0.5453 mL | 1.3632 mL | |
| 50 mM | 0.0436 mL | 0.2181 mL | 0.4362 mL | 1.0906 mL | |
| 60 mM | 0.0364 mL | 0.1818 mL | 0.3635 mL | 0.9088 mL | |
| 80 mM | 0.0273 mL | 0.1363 mL | 0.2726 mL | 0.6816 mL | |
| 100 mM | 0.0218 mL | 0.1091 mL | 0.2181 mL | 0.5453 mL |
HPK1-IN-7 Related Classifications
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