SJ6986 是有效的、选择性的、口服有效的 GSPT1/2 降解剂，其对GSPT1 的DC50 值为2.1 nM (Dmax 99%)。
货号:ajcx33484
CAS:N/A
分子式:C20H14F3N3O7S
分子量：497.4
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

SJ6986 is a potent, selective and orally active GSPT1/2 degrader, with a DC50 of 2.1 nM (Dmax 99%) for GSPT1[1].

SJ6986 exhibits EC50 values of 1.5 nM, 0.4 nM, 726 nM, 336 nM and 3583 nM in MV4-11, MHH-CALL-4, MB002, MB004 and HD-MB03 cell lines, respectively[1].

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].

[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.