| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
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| Targets |
IC50: 5 nM (GCN2)[1]
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|---|---|
| ln Vitro |
T cell proliferation is restored and myeloid-derived suppressive cells (MDSC)-related T cell suppression is lessened by GCN2-IN-7 (600 nM; 3 d)[1].
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| ln Vivo |
At a suitable dosage, GCN2-IN-7 (oral gavage; 15 mg/kg; BID; 17 d) exhibits strong target engagement in vivo[1]. In the LL2 syngeneic mouse tumor model, GCN2-IN-7 (oral gavage; 50 mg/kg; BID; 17 d) suppresses tumor growth in vivo[1].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: CD8+ T cells from WT and GCN2KO cells Tested Concentrations: 600 nM Incubation Duration: 3 days Experimental Results: Relieved MDSC suppression of proliferation of the co-cultured CD8+ T cells with significant relief at 600 nM. |
| Animal Protocol |
Animal/Disease Models: balb/c (Bagg ALBino) mouse injected with RENCA cells[1]
Doses: 15 mg/kg Route of Administration: Oral gavage; 15 mg/kg; BID; 17 days Experimental Results: demonstrated robust target engagement of GCN2 in both tumor (average of 84%) and spleen (average of 80%) tissues. demonstrated an average of 65% reduction of downstream marker Activation Transcription Factor 4 (ATF4) in compound-treated mice compared to the vehicle treatment group. Animal/Disease Models: LL2 syngeneic mouse model[1] Doses: 50 mg/kg Route of Administration: Oral gavage; 50 mg/kg; BID; 17 days Experimental Results: demonstrated tumor growth inhibition (56%) after 26 days of dosing compared to the vehicle group. |
| References |
[1]. Jackson JJ, et al. Potent GCN2 Inhibitor Capable of Reversing MDSC-Driven T Cell Suppression Demonstrates In Vivo Efficacy as a Single Agent and in Combination with Anti-Angiogenesis Therapy. J Med Chem. 2022 Sep 20.
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| Molecular Formula |
C22H23BRN8OS
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|---|---|
| Molecular Weight |
527.44
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| CAS # |
2396465-33-9
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
[C@]1(C)(C(NC)=O)CC[C@@H](NC2=NC=C3C(Br)=NN(C4=CC=C(C5=NN=C(C)S5)C=C4)C3=N2)C1
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 50 mg/mL (94.80 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.74 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8960 mL | 9.4798 mL | 18.9595 mL | |
| 5 mM | 0.3792 mL | 1.8960 mL | 3.7919 mL | |
| 10 mM | 0.1896 mL | 0.9480 mL | 1.8960 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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