Figure 5 from Targeted Degradation of SOS1 Exhibits Potent Anticancer Activity and Overcomes Resistance in KRAS-Mutant Tumors and BCR–ABL–Positive Leukemia

作者：Ziwei Luo, Chencen Lin, Chuwei Yu, Changxian Yuan, Wenyong Wu, Xiaowei Xu, Renhong Sun, Yan Jia, Yafang Wang, Jie Shen, Dingyan Wang, Sinan Wang, Hualiang Jiang, Biao Jiang, Xiaobao Yang, Chengying Xie · 年份：2025 · DOI：10.1158/0008-5472.28122532 · 研究领域：Chronic Myeloid Leukemia Treatments、Chronic Lymphocytic Leukemia Research、Acute Lymphoblastic Leukemia research

SIAIS562055 inhibits the proliferation of CML cells in vitro. A, Western blot analysis of SOS1 in K562 cells treated with SIAIS562055 (1,000 nmol/L), SIAIS562092 (1,000 nmol/L), or BI-3406 (1,000 nmol/L) for 24 hours, with or without the pretreatment of MG132 (1,000 nmol/L) for 1 hour. B, Western blot analysis of SOS1, pERK, GSPT1, and IKZF3 in K562 cells treated with SIAIS562055, SIAIS562092, or BI-3406 for 24 hours. C, Western blot analysis of SOS1 and pERK in K562 cells treated with a time gradient of SIAIS562055 or SIAIS562092. Histogram shows the relative SOS1 levels. D, Western blot analysis of SOS1 and pERK in K562 cells treated with SIAIS562055 (1,000 nmol/L), SIAIS562092 (1,000 nmol/L), or BI-3406 (1,000 nmol/L) for 12 hours, followed by wash-out and incubation with fresh media for another 0, 24, 48, and 72 hours. Line chart shows the relative pERK levels. E, Western blot analysis of SOS1 and pERK in K562 and KU812 cells treated with SIAIS562055 for 24 hours in a concentration gradient. F, Antiproliferative effects in K562 and KU812 cells after treatment with SIAIS562055 for 72 hours. Line charts show the IC50 values of two-dimensional culture. Data are shown as mean ± SD, n = 3. **, P < 0.01; ***, P < 0.001; ns, not significant.