ALW-II-41-27

• CAT Number: I000666
• CAS Number: 1186206-79-0
• Molecular Formula: C32H32F3N5O2S
• Molecular Weight: 607.69
• Purity: ≥95%
• Synonyms: N-(5-((4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)carbamoyl)-2-methylphenyl)-5-(thiophen-2-yl)nicotinamide
• Target: Ephrin Receptor
• Solubility: DMSO 47 mg/ml
• Storage: Store at -20°C
• IC50: 11 nM to EPHA2
• SMILES: CCN1CCN(CC2=C(C(F)(F)F)C=C(NC(C3=CC(NC(C4=CN=CC(C5=CC=CS5)=C4)=O)=C(C=C3)C)=O)C=C2)CC1

ALW-II-41-27 (CAT: I000666) is indeed a potent inhibitor of EPH family kinases, particularly EPHA2. It has demonstrated an IC50 value of 11 nM for inhibiting the activity of EPHA2. The EPH family of receptor tyrosine kinases plays crucial roles in various cellular processes, including cell adhesion, migration, and signaling. By selectively targeting EPHA2, ALW-II-41-27 may have potential applications in cancer research and therapy, as aberrant EPHA2 signaling has been implicated in tumor progression and metastasis. Further investigation is necessary to explore its therapeutic potential and selectivity profile.

Reference

[1]. Choi, Yongmun; Syeda, Farisa; Walker, John R.; Finerty, Patrick J.; Cuerrier, Dominic; Wojciechowski, Amy; Liu, Qingsong; Dhe-Paganon, Sirano; Gray, Nathanael S. Discovery and structural analysis of Eph receptor tyrosine kinase inhibitors. Bioorganic & Medicinal Chemistry Letters (2009), 19(15), 4467-4470.
[2]. Lisle JE, Mertens-Walker I, Rutkowski R, et al. Eph receptors and their ligands: Promising molecular biomarkers and therapeutic targets in prostate cancer. Biochim Biophys Acta. 2013 Feb 8;1835(2):243-257. doi: 10.1016/j.bbcan.2013.01.003.
[3]. Salvucci O, Tosato G. Essential roles of EphB receptors and EphrinB ligands in endothelial cell function and angiogenesis. Adv Cancer Res. 2012;114:21-57. doi: 10.1016/B978-0-12-386503-8.00002-8.
[4]. Chen J. Regulation of tumor initiation and metastatic progression by Eph receptor tyrosine kinases. Adv Cancer Res. 2012;114:1-20. doi: 10.1016/B978-0-12-386503-8.00001-6.