SI-109 is a potent STAT3 SH2 domain inhibitor (K i =9 nM) with antitumor activity. SI-109 effectively inhibits the transcriptional activity of STAT3 (IC 50 =3 μM). SI-109 and an analog of CRBN ligand lenalidomide have been used to design PROTAC STAT3 degrader SD-36.
性状
Solid
IC50 & Target[1][2]
STAT3 9 nM (Ki)
体外研究(In Vitro)
SI-109 exerts a moderate growth inhibitory activity in MOLM-16 cells (IC50=3 μM).SI-109 is ineffective in inhibition of STAT3 Y705 phosphorylation and in suppression of c-Myc expression at concentrations as high as 10 μM. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献
[1]. Bai L, et al. A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo. Cancer Cell. 2019 Nov 11;36(5):498-511.e17.
溶解度数据
In Vitro: DMSO : 150 mg/mL (179.47 mM; Need ultrasonic)配制储备液