Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK6853 is a potent, soluble, cell-active, and highly selective inhibitor of the BRPF1 bromodomain.
説明 | GSK6853 is a potent, soluble, cell-active, and highly selective inhibitor of the BRPF1 bromodomain. |
ターゲット&IC50 | BRPF1:8.1(pIC50) |
In vitro | Screening GSK6853 against a panel of 48 unrelated assays reveals only off-target activities that are relatively weak compared to the BRPF1 potency. However, to minimize the chance of off-target effects , the recommended concentration is no higher than 1 μM in cell-based assays[1]. |
In vivo | In male CD1 mouse, following IV administration (1 mg/kg), GSK6853 demonstrates a high blood clearance of 107 mL/min/kg, a moderate volume of distribution (5.5 L/kg) and a moderate terminal half-life of 1.7 h. Oral administration (PO, 3 mg/kg) achieves a moderate systemic exposure, with a Cmax of 42 ng/mL and Tmax of 1.5 h, resulting in a bioavailability of 22%. The intraperitoneal route of administration (IP, 3 mg/kg) reaches a Cmax of 469 ng/mL and Tmax of 0.25 h, resulting in a bioavailability of 85%. The results indicate that the IP route of administration would be suitable for dosing this molecule in potential PKPD models[1]. |
分子量 | 409.48 |
分子式 | C22H27N5O3 |
CAS No. | 1910124-24-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (134.41 mM)
Ethanol: 81 mg/mL (197.81 mM)
You can also refer to dose conversion for different animals. 詳細
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
GSK6853 1910124-24-1 Chromatin/Epigenetic Epigenetic Reader Domain Inhibitor inhibit GSK 6853 GSK-6853 inhibitor