| CAS NO: | 1910124-24-1 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 409.48 |
|---|---|
| Formula | C22H27N5O3 |
| CAS No. | 1910124-24-1 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 81 mg/mL warmed (197.81 mM) |
| Water: <1 mg/mL | |
| Ethanol: 81 mg/mL warmed (197.81 mM) | |
| SMILES | O=C(NC1=C(N2[C@H](C)CNCC2)C=C(N3C)C(N(C)C3=O)=C1)C4=CC=CC=C4OC |
| Synonyms | GSK6853; GSK 6853; GSK-6853 |
| In Vitro | In vitro activity: 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. Kinase Assay: GSK6853 is a novel, potent and selective benzimidazolone BRPF1 bromodomain inhibitor with pIC50 of 8.1 (TR-FRET) and showed greater than 1600-fold selectivity over all other bromodomains tested. The BRPF (Bromodomain and PHD Finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. 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. Cell Assay: |
|---|---|
| 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. |
| Animal model | CD1 mice |
| Formulation & Dosage | 1 mg/kg (i.v); i.v, p.o, i.p |
| References | ACS Med Chem Lett. 2016 May 9;7(6):552-7 |
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