[CAS NO. 2183470-09-7] GCN2-IN-6
PRODUCTS SPECIFICATIONS [2183470-09-7]
DESCRIPTION [2183470-09-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 485.29 |
| Molecular Formula | C19H12Cl2F2N4O3S |
| SMILES | O=S(C1=CC(Cl)=CC(CO)=C1Cl)(NC2=CC=C(F)C(C#CC3=CN=C(N)N=C3)=C2F)=O |
2 Publications Citing Use of MCE
Summary
IC50 & Target
IC50: 1.8 nM (GCN2, in-house enzymatic) and 9.3 nM (GCN2, cellular assays); 0.26 nM (PERK, in-house enzymatic) and 230 nM (PERK, cellular assays) [1]
In Vitro
To examine the impact of GCN2 inhibition on cancer cell proliferation, acute lymphoblastic leukemia (ALL) CCRFCEM cells are treated with GCN2-IN-6 (Compound 6d) in the presence of asparaginedepleting agent asparaginase. Treatment with GCN2-IN-6 greatly sensitizes CCRF-CEM cells to asparaginase. The moderate antiproliferative effects achieved by combining asparaginase and GCN2-IN-6 treatment are observed in GCN2-wildtype (WT) mouse embryonic fibroblast (MEF) cells but not in GCN2-knockout (KO) MEF. GCN2-IN-6 demonstrates suppression on p-GCN2, p-eIF2α, and ATF4 activated by asparaginase [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
GCN2-IN-6 (Compound 6d; 0.3-3 mg/kg; oral administration; for 8 hours; mice) treatment at 3 mg/kg suppresses both self-phosphorylation of GCN2 and the downstream effector ATF4 to the basal level following pretreatment with asparaginase [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Mice bearing CCRF-CEM cells xenografts [1] |
| Dosage: | 0.3 mg/kg, 1 mg/kg, and 3 mg/kg |
| Administration: | Oral administration; for 8 hours |
| Result: | Suppressed both self-phosphorylation of GCN2 and the downstream effector ATF4 to the basal level following pretreatment with asparaginase. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 250 mg/mL ( 515.16 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.29 mM); Clear solution