Tilfrinib is a selective Brk/PTK6 inhibitor with an IC₅₀ value of 3.15nM for Brk[1-2]. Tilfrinib is primarily used in cancer-related research[3-4].
In vitro, Tilfrinib (0-20μM) was administered to human lung adenocarcinoma cell lines PC9 and H1975 for 24-48 hours. Tilfrinib significantly inhibited PTK6 protein expression and reduced cell viability in a dose-dependent manner. Tilfrinib also suppressed colony formation, migration, and invasion capabilities in PC9 and H1975 cells, and induced apoptosis. Tilfrinib upregulated PD-L1 expression in the treated cells[4]. ETV4 WT-induced UM-UC-3 cells were treated with Tilfrinib (20μM) for 36 hours. Tilfrinib inhibited PTK6 and reduced the expression of CXCL1 or CXCL8 in cells[5].
References:
[1] Mahmoud KA, Krug M, Wersig T, et al. Discovery of 4-anilino α-carbolines as novel Brk inhibitors. Bioorg Med Chem Lett. 2014 Apr 15;24(8):1948-51.
[2] Chen B, Liu B, Chen J, et al. PTK6 drives HNRNPH1 phase separation to activate autophagy and suppress apoptosis in colorectal cancer. Autophagy. 2025 Aug;21(8):1680-1699.
[3] Jerin S, Harvey AJ, Lewis A. Therapeutic Potential of Protein Tyrosine Kinase 6 in Colorectal Cancer. Cancers (Basel). 2023 Jul 21;15(14):3703.
[4] Xiong RH, Yang SQ, Li JW, et al. Identification of immune-associated biomarker for predicting lung adenocarcinoma: bioinformatics analysis and experiment verification of PTK6. Discov Oncol. 2024 Apr 4;15(1):102.
[5] Zhang Q, Liu S, Wang H, et al. ETV4 Mediated Tumor-Associated Neutrophil Infiltration Facilitates Lymphangiogenesis and Lymphatic Metastasis of Bladder Cancer. Adv Sci (Weinh). 2023 Apr;10(11):e2205613.
Tilfrinib是一种选择性的Brk/PTK6抑制剂，对Brk的IC50值为3.15nM[1]。Tilfrinib主要用于癌症相关的研究[2-3]。
在体外，Tilfrinib（0-20μM）处理人肺腺癌细胞PC9和H1975细胞24-48小时，Tilfrinib显著抑制PTK6蛋白表达，并以剂量依赖的方式降低细胞活力。Tilfrinib抑制了PC9和H1975细胞的克隆形成、迁移和侵袭能力，诱导细胞凋亡。Tilfrinib还上调了细胞PD-L1的表达[4]。Tilfrinib（20μM）处理ETV4 WT诱导的UM-UC-3细胞和TAN细胞36小时，Tilfrinib可抑制PTK6，并降低细胞中CXCL1或CXCL8表达[5]。