| CAS NO: | 1619994-68-1 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 371.45 |
|---|---|
| Formula | C20H21NO4S |
| CAS No. | 1619994-68-1 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 74 mg/mL (199.2 mM) |
| Water: <1 mg/mL | |
| Ethanol: 7 mg/mL (18.8 mM) | |
| Solubility (In vivo) | 0.5% CMC+1% Tween 80: 30mg/mL |
| Synonyms | GSK-2801; GSK 2801; GSK2801 Chemical Name: 1-(1-(2-(methylsulfonyl)phenyl)-7-propoxyindolizin-3-yl)ethanone InChi Key: KHWCPNJRJCNVRI-UHFFFAOYSA-N InChi Code: InChI=1S/C20H21NO4S/c1-4-11-25-15-9-10-21-18(14(2)22)13-17(19(21)12-15)16-7-5-6-8-20(16)26(3,23)24/h5-10,12-13H,4,11H2,1-3H3 SMILES Code: CC(C1=CC(C2=CC=CC=C2S(=O)(C)=O)=C3C=C(OCCC)C=CN13)=O |
| In Vitro | In vitro activity: In U2OS cells transfected with mutant BAZ2A (N1873F), GSK2801 (1 μM) accelerates FRAP half-recovery time by displacing BAZ2A from chromatin. Kinase Assay: GSK2801 is a potent, selective and cell active acetyl-lysine competitive inhibitor of BAZ2A(Kd=136 nM) and BAZ2B(Kd=257 nM) bromodomains. Cell Assay: In U2OS cells, treatment with the SAHA induced hyperacetylated chromatin. In a GFP-BAZ2A fusion construct, the conserved asparagines that are essential for recognizing the acetylated lysine has been mutated. When a GFP-BAZ2A fusion construct was transfected into SAHA-treated U2OS cells, the mutant construct accelerated FRAP half-recovery time. Treatment with GSK2801 alone in U2OS cells also accelerated FRAP half-recovery time. Both acceleration extents are the same. This meant that GSK2801 can displace BAZ2A from chromatin. |
|---|---|
| In Vivo | In male CD1 mice, GSK2801 (30 mg/kg, p.o. and i.p.) has reasonable in vivo exposure after oral dosing, modest clearance, and reasonable plasma stability. |
| Animal model | Male CD1 mice |
| Formulation & Dosage | Formulated in 0.5% CMC+1% Tween 80; 30 mg/kg; i.p. or p.o. |
| References | J Med Chem. 2016 Feb 25;59(4):1410-24. |
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