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

SJ6986 demonstrates potency with EC50 values at 1.5 nM, 0.4 nM, 726 nM, 336 nM, and 3583 nM in the MV4-11, MHH-CALL-4, MB002, MB004, and HD-MB03 cell lines respectively [1]. In MV4-11 cells, under conditions of a 0-100 μM concentration range and a 3-day incubation, an EC50 of 1.5 nM was observed, indicating significant inhibition of cell proliferation [1]. Additionally, Western Blot analysis in the same cell line, with a concentration range of 0-10 μM over 4 and 24 hours, revealed a dose- and time-dependent reduction in GSPT1 protein levels, further confirming the compound's efficacy [1].

SJ6986 shows t 1/2 of 3.44 h by intravenous injection of 3 mg/kg and t max of 0.25 h by oral administration (%F = 84) of 10 mg/kg in CD1 mice [1].