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GSK2606414
| Product Name | GSK2606414 |
| Price: | Inquiry |
| Catalog No.: | CN00451 |
| CAS No.: | 1337531-36-8 |
| Molecular Formula: | C24H20F3N5O |
| Molecular Weight: | 451.44 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | O=C(N1CCc2c1ccc(c2)c1cn(c2c1c(N)ncn2)C)Cc1cccc(c1)C(F)(F)F |
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| Description | GSK2606414 is a cell-permeable and orally available PERK inhibitor with an IC50 of 0.4 nM. |
| Target | EIF2AK3 (PERK):0.4 nM (IC50) EIF2AK1 (HRI):420 nM (IC50) EIF2AK2 (PKR):696 nM (IC50) |
| In Vitro | GSK2606414 inhibits PERK activation in cells[1]. |
| In Vivo | GSK2606414 (50 and 150 mg/kg, p.o.) inhibits the growth of a human tumor xenograft in mice[1]. |
| Animal Admin | Exponentially growing BxPC3 tumor cells (10×106 cells/mouse) from cell culture are implanted subcutaneously into the right flank of female nude mice. Sixteen days after implantation, mice with -200 mm3 tumors are randomized into various treatment groups (n=8 mice/group). Animals are orally treated with vehicle (0.5% hydoxypropylmethylcellulose, 0.1% Tween 80 in water, pH 4.8), compound at 50 or 150 mg/kg, b.i.d. for 21 days. Tumor volume is measured twice weekly with calipers and calculated. Results are represented as percent inhibition on completion of dosing, which is 100[1-(average growth of drug-treated population)/(average growth of vehicle-treated control population)]. Statistical analysis is performed using a two-tailed t test. |
| Density | 1.4±0.1 g/cm3 |
| Boiling Point | 720.3±60.0 °C at 760 mmHg |
| Flash Point | 389.4±32.9 °C |
| Exact Mass | 451.161987 |
| PSA | 77.04000 |
| LogP | 4.53 |
| Vapour Pressure | 0.0±2.3 mmHg at 25°C |
| Storage condition | -20°C |