GCN2-IN-7
Based on 2 publication(s) in Google Scholar
GCN2-IN-7 (compound 39) is an orally active and selective general control nonderepressible 2 (GCN2) inhibitor (IC50=5 nM). GCN2-IN-7 shows anti-tumor activity in vivo.
For research use only. We do not sell to patients.
- Purity: 99.92%
- CAS No.: 2396465-33-9
- Formula: C22H23BrN8OS
- Molecular Weight:527.44
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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)
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) GCN2-IN-7
More
Biological Activity
IC50: 5 nM (GCN2)[1]
GCN2-IN-7 (600 nM; 3 d) alleviates myeloid-derived suppressive cells (MDSC)-related T cell suppression and restores T cell proliferation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CD8+ T cells from WT and GCN2KO cells
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Concentration:600 nM
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Incubation Time:3 days
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Result:Relieved MDSC suppression of proliferation of the co-cultured CD8+ T cells with significant relief at 600 nM.
GCN2-IN-7 (oral gavage; 50 mg/kg; BID; 17 d) inhibits tumor growth in vivo of the LL2 syngeneic mouse tumor model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c mice injected with RENCA cells[1]
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Dosage:15 mg/kg
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Administration:Oral gavage; 15 mg/kg; BID; 17 days
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Result:Showed robust target engagement of GCN2 in both tumor (average of 84%) and spleen (average of 80%) tissues.
Showed an average of 65% reduction of downstream marker Activation Transcription Factor 4 (ATF4) in compound-treated mice compared to the vehicle treatment group.
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Animal Model:LL2 syngeneic mouse model[1]
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Dosage:50 mg/kg
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Administration:Oral gavage; 50 mg/kg; BID; 17 days
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Result:Showed tumor growth inhibition (56%) after 26 days of dosing compared to the vehicle group.
Chemical Information
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CAS No. 2396465-33-9
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Appearance Solid
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Molecular Weight 527.44
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Formula C22H23BrN8OS
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Color White to off-white
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SMILES
O=C([C@@]1(C)C[C@H](NC2=NC=C3C(N(C4=CC=C(C5=NN=C(C)S5)C=C4)N=C3Br)=N2)CC1)NC
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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)
Publications (2)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
DMSO : 50 mg/mL (94.80 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 (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.
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.
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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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.
Purity & Documentation
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Data Sheet (277 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8960 mL | 9.4798 mL | 18.9595 mL | 47.3988 mL |
| 5 mM | 0.3792 mL | 1.8960 mL | 3.7919 mL | 9.4798 mL | |
| 10 mM | 0.1896 mL | 0.9480 mL | 1.8960 mL | 4.7399 mL | |
| 15 mM | 0.1264 mL | 0.6320 mL | 1.2640 mL | 3.1599 mL | |
| 20 mM | 0.0948 mL | 0.4740 mL | 0.9480 mL | 2.3699 mL | |
| 25 mM | 0.0758 mL | 0.3792 mL | 0.7584 mL | 1.8960 mL | |
| 30 mM | 0.0632 mL | 0.3160 mL | 0.6320 mL | 1.5800 mL | |
| 40 mM | 0.0474 mL | 0.2370 mL | 0.4740 mL | 1.1850 mL | |
| 50 mM | 0.0379 mL | 0.1896 mL | 0.3792 mL | 0.9480 mL | |
| 60 mM | 0.0316 mL | 0.1580 mL | 0.3160 mL | 0.7900 mL | |
| 80 mM | 0.0237 mL | 0.1185 mL | 0.2370 mL | 0.5925 mL |
GCN2-IN-7 Related Classifications
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