| Bioactivity | SJ6986 is a potent, selective and orally active GSPT1/2 degrader, with a DC50 of 2.1 nM (Dmax 99%) for GSPT1[1]. | ||||||||||||
| Target | DC50: 2.1 nM (GSPT1). | ||||||||||||
| Invitro | 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]. Cell Proliferation Assay[1] Cell Line: | ||||||||||||
| 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]. | ||||||||||||
| Name | SJ6986 | ||||||||||||
| CAS | 2765625-93-0 | ||||||||||||
| Formula | C20H14F3N3O7S | ||||||||||||
| Molar Mass | 497.40 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |