Description
SJ6986 is a Potent, Selective, and Orally Bioavailable Small-Molecule GSPT1/2 Degrader from a Focused Library of Cereblon Modulator.
Uses
SJ6986 is a potent, selective and orally active GSPT1/2 Molecular Glue degrader, with a DC50 of 2.1 nM (Dmax 99%) for GSPT1[1].
in vivo
SJ6986 exhibits t1/2 of 3.44 h by iv injection of 3 mg/kg and tmax of 0.25 h by oral administration (%F = 84) of 10 mg/kg in CD1 mice[1].
References
[1] Gisele Nishiguchi, et al. Identification of Potent, Selective, and Orally Bioavailable Small-Molecule GSPT1/2 Degraders from a Focused Library of Cereblon Modulators. J Med Chem. 2021 May 27. DOI:
10.1021/acs.jmedchem.0c01313
