GNE-6893
Based on 1 Customer Validation
GNE-6893 is an orally active, selective HPK1 inhibitor with a Ki < 0.02 nM. GNE-6893 enhances T cell receptor signaling in primary human T cells. GNE-6893 increases IL2 production in stimulated primary human T cells. GNE-6893 can be used for the research of chronic refractory cancers.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.94%
- No. CAS: 2415374-98-8
- Fòrmula: C23H24FN5O4
- Peso molecular:453.47
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Almacenamiento: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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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HPK1 |
IL-2 |
GNE-6893 inhibits anti-CD3/anti-CD28-induced phosphorylation of SLP76 in Jurkat cells with an IC50 of 44 nM[1].
GNE-6893 (0.001-10 μM) enhances IL2 secretion in primary human T cells stimulated with anti-CD3/anti-CD28, with an IL2 EC50 of 6.4 nM[1].
GNE-6893 (100 nM) inhibits the activity of 8 kinases by more than 50%, with the strongest off-target activity against GLK (IC50 of 0.72 nM) and GCK (IC50 of 1.3 nM), and weaker activity against Aurora B (IC50 of 46 nM) and LRRK2 (IC50 of 31 nM)[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:C57BL/6 mice; Sprague-Dawley rats; Beagle dogs; Cynomolgus monkeys[1]
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Dosage:1 mg/kg (mouse, i.v.); 25 mg/kg (mouse, p.o.); 0.5 mg/kg (rat, i.v.); 0.5 mg/kg (dog, i.v.); 0.5 mg/kg (dog, p.o.); 0.5 mg/kg (cynomolgus monkey, i.v.); 0.5 mg/kg (cynomolgus monkey, p.o.)
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Administration:i.v.; p.o.
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Result:Exhibited plasma clearance of 34 mL/min/kg, volume of distribution at steady state (Vss) of 1.8 L/kg, half-life (t1/2) of 1.7 h, and oral bioavailability of 37% (mouse).
Exhibited plasma clearance of 39 mL/min/kg, Vss of 2.2 L/kg, t1/2 of 1.3 h, and oral bioavailability of 30% (rat).
Exhibited plasma clearance of 14 mL/min/kg, Vss of 2.2 L/kg, t1/2 of 2.5 h, and oral bioavailability of 46% (dog).
Exhibited plasma clearance of 14 mL/min/kg, Vss of 1.9 L/kg, t1/2 of 1.9 h, and oral bioavailability of 53% (cynomolgus monkey).
Chemical Information
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No. CAS 2415374-98-8
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Appearance Solid
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Peso molecular 453.47
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Fòrmula C23H24FN5O4
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Color Off-white to light yellow
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SMILES
FC1=C(N)C(C=NC(NC(O[C@@H]2[C@H](COC2)C)=O)=C3)=C3C=C1C4=CN=C(OCCN5)C5=C4C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (220.52 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)
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.
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.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.2052 mL | 11.0261 mL | 22.0522 mL | 55.1304 mL |
| 5 mM | 0.4410 mL | 2.2052 mL | 4.4104 mL | 11.0261 mL | |
| 10 mM | 0.2205 mL | 1.1026 mL | 2.2052 mL | 5.5130 mL | |
| 15 mM | 0.1470 mL | 0.7351 mL | 1.4701 mL | 3.6754 mL | |
| 20 mM | 0.1103 mL | 0.5513 mL | 1.1026 mL | 2.7565 mL | |
| 25 mM | 0.0882 mL | 0.4410 mL | 0.8821 mL | 2.2052 mL | |
| 30 mM | 0.0735 mL | 0.3675 mL | 0.7351 mL | 1.8377 mL | |
| 40 mM | 0.0551 mL | 0.2757 mL | 0.5513 mL | 1.3783 mL | |
| 50 mM | 0.0441 mL | 0.2205 mL | 0.4410 mL | 1.1026 mL | |
| 60 mM | 0.0368 mL | 0.1838 mL | 0.3675 mL | 0.9188 mL | |
| 80 mM | 0.0276 mL | 0.1378 mL | 0.2757 mL | 0.6891 mL | |
| 100 mM | 0.0221 mL | 0.1103 mL | 0.2205 mL | 0.5513 mL |
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