SJ6986 是有效的、选择性的、具有口服活性的GSPT1/2降解剂,对GSPT1 的DC50值为2.1 nM (Dmax99%)。
产品描述
SJ6986 is a potent, selective and orally active GSPT1/2 degrader. SJ6986 degrades GSPT1 with a DC 50 of 2.1 nM (D max 99%) [1].
体外活性
SJ6986 shows EC 50 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: MV4-11 cells. Concentration: 0-100 μM. Incubation Time: 3 days. Result: Exhibited EC 50 of 1.5 nM. Western Blot Analysis [1] Cell Line: MV4-11 cells. Concentration: 0-10 μM. Incubation Time: 4 and 24 h. Result: Dose- and time-dependently decreased the protein levels of GSPT1.
体内活性
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].
Cas No.
2765625-93-0
分子式
C20H14F3N3O7S
分子量
497.4
别名
SJ6986
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years