| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
GCN2
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|---|---|
| ln Vitro |
In acute lymphoblastic leukemia (ALL) CCRFCEM cells, GCN2-IN-6 (compound 6d) was applied in the presence of asparaginase, an asparagine-depleting agent, to investigate the impact of GCN2 inhibition on cancer cell proliferation. The CCRF-CEM cells' sensitivity to asparaginase was significantly enhanced by treatment with GCN2-IN-6. GCN2 wild-type (WT) mouse embryonic fibroblasts (MEFs) showed a slight antiproliferative impact from combined asparaginase and GCN2-IN-6 treatment, while GCN2 knockout (KO) MEFs did not show this effect. ATF4, p-eIF2α, and GCN2-IN-6 are all inhibited by asparaginase[1].
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| ln Vivo |
GCN2-IN-6 (Compound 6d; 0.3-3 mg/kg; oral) at 3 mg/kg suppresses the autophosphorylation of GCN2 and the downstream effector ATF4 to basal levels following asparaginase pretreatment [1].
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| Animal Protocol |
Animal/Disease Models: Mice bearing CCRF-CEM cells xenografts[1]
Doses: 0.3 mg/kg, 1 mg/kg, and 3 mg/kg Route of Administration: Oral administration; for 8 hrs (hours) Experimental Results: Suppressed both self-phosphorylation of GCN2 and the downstream effector ATF4 to the basal level following pretreatment with asparaginase. |
| References |
[1]. Fujimoto J, et al. Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type I Half Binding Mode. ACS Med Chem Lett. 2019 Sep 19;10(10):1498-1503.
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| Molecular Formula |
C19H12CL2F2N4O3S
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|---|---|
| Molecular Weight |
485.29
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| CAS # |
2183470-09-7
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| SMILES |
ClC1C(CO)=CC(=CC=1S(NC1C=CC(=C(C#CC2=CN=C(N)N=C2)C=1F)F)(=O)=O)Cl
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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 : 250 mg/mL (515.16 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.29 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.29 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 20.8 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 | 2.0606 mL | 10.3031 mL | 20.6062 mL | |
| 5 mM | 0.4121 mL | 2.0606 mL | 4.1212 mL | |
| 10 mM | 0.2061 mL | 1.0303 mL | 2.0606 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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