For research use only. Not for therapeutic Use.
GSK973 is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5)[1].
GSK973 (1 mg/kg; i.v.) treatment shows the CL, CIrenal, Vss, and T1/2 are 73 mL/min/kg, 4 mL/min/kg, 2.1L/kg, and 0.6 hours, respectively[1].
GSK973 (3 mg/kg; p.o) treatment shows the Fpo of 48%[1].
| Catalog Number | I044616 |
| CAS Number | 2138473-38-6 |
| Synonyms | (2S,3S)-2-(fluoromethyl)-7-N-methyl-5-N-[(1R,5S)-3-oxabicyclo[3.1.0]hexan-6-yl]-3-phenyl-2,3-dihydro-1-benzofuran-5,7-dicarboxamide |
| Molecular Formula | C23H23FN2O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C23H23FN2O4/c1-25-23(28)15-8-13(22(27)26-20-16-10-29-11-17(16)20)7-14-19(12-5-3-2-4-6-12)18(9-24)30-21(14)15/h2-8,16-20H,9-11H2,1H3,(H,25,28)(H,26,27)/t16-,17+,18-,19+,20?/m1/s1 |
| InChIKey | WZQLVEPIBAOOGF-SFDMMAKQSA-N |
| SMILES | CNC(=O)C1=CC(=CC2=C1OC(C2C3=CC=CC=C3)CF)C(=O)NC4C5C4COC5 |
| Reference | [1]. Preston A, et al. GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family. ACS Med Chem Lett. 2020;11(8):1581-1587. Published 2020 Jul 6. |
