SI-109是一种有效的STAT3SH2domain结构域抑制剂(Ki=9nM)，具有抗肿瘤活性。SI-109有效抑制STAT3的转录活性(IC50=3μM)。SI-109和CRBN类似物lenalidomide配体用于设计PROTACSTAT3降解剂SD-36。
货号:ajcx31466
CAS:2429877-30-3
分子式:C40H44F2N7O9P
分子量：835.79
溶解度:DMSO: 150 mg/mL (179.47 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

SI-109 is a potent STAT3 SH2 domain inhibitor (Ki=9 nM) with antitumor activity. SI-109 effectively inhibits the transcriptional activity of STAT3 (IC50=3 μM). SI-109 and an analog of CRBN ligand lenalidomide have been used to design PROTAC STAT3 degrader SD-36[1].

SI-109 exerts a moderate growth inhibitory activity in MOLM-16 cells (IC50=3 μM)[1].SI-109 is ineffective in inhibition of STAT3 Y705 phosphorylation and in suppression of c-Myc expression at concentrations as high as 10 μM[1].

[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.