Name: ALW-II-41-27
Price: 446.00 USD

- Overview
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    Background
    
    ALW-II-41-27 is a potent inhibitor of EPH family kinases, with an IC50 value of 11 nM to EPHA2 [1] [2].
    EPH family proteins are key regulators of both disease and normal development. EPH receptors are involved in many intracellular signaling pathways such as PI3K/AKT/mTOR, RAS/RAF/MAPK, FAK, SRC, ABL, and RHO/RAC/CDC42 [2].
    In H358 cells, treatment with ALW-II-41-27 at a concentration of 1 μM within 15 minutes impaired the tyrosine phosphorylation of the EPHA2 receptor and continued to inhibit the tyrosine phosphorylation through 6 hours. ALW-II-41-27 also dose-dependently inhibited the EPHA2 phosphorylation induced by ligand. When the EPHA2 was depleted by RNAi in NSCLC cell lines, cells were much less sensitive to ALW-II-41-27.
    It was suggested that EPHA2 plays an oncogenic role according to results in lung cancers. In mice bearing non–small cell lung cancers (NSCLCs), intraperitoneal injection with ALW-II-41-27 at a dose of 15 mg/kg twice daily for 14 days significantly resulted in an inhibition of the growth of H358 tumors. ALW-II-41-27 significantly increased the apoptosis of tumors compared with the vehicle alone or NG-25. This was similar to the effect of the genetic ablation of EPHA2. Compared with treatments with vehicle alone or NG-25, treatment with ALW-II-41-27 did not result in significant differences in the vessel density or proliferation of tumors [2].
    
    [1]. Marialuisa Moccia, Qingsong Liu, Teresa Guida, et al. Identification of Novel Small Molecule Inhibitors of Oncogenic RET Kinase. PLOS ONE, 2015, 10(6):e0128364.
    [2]. Katherine R. Amato, Shan Wang, Andrew K. Hastings, et al. Genetic and pharmacologic inhibition of EPHA2 promotes apoptosis in NSCLC. Journal of Clinical Investigation, 2014, 124(5):2037-2049.
- Properties
  - Alternative Name
    
    Eph receptor tyrosine kinase inhibitor;; N-(5-((4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)carbamoyl)-2-methylphenyl)-5-(thiophen-2-yl)nicotinamide
    
    CAS Number
    
    1186206-79-0
    
    Molecular Formula
    
    C32H32F3N5O2S
    
    Molecular Weight
    
    607.69
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥60.8 mg/mL in EtOH; insoluble in H2O; ≥102 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Yutuan Wu, Jie Huang, et al. "MEK inhibition overcomes resistance to EphA2-targeted therapy in uterine cancer." Gynecol Oncol. 2021 Oct;163(1):181-190. PMID:34391578
    2. Hao Wang, Wei Hou, et al. "Targeting EphA2 suppresses hepatocellular carcinoma initiation and progression by dual inhibition of JAK1/STAT3 and AKT signaling." Cell Rep. 2021 Feb 23;34(8):108765. PMID:33626345
    3. Tessa Y.S. Le Large, Elisa Giovannetti, et al. "Microdissected pancreatic cancer proteomes reveal tumor heterogeneity and therapeutic targets." JCI Insight. 2020;5(15):e138290. PMID:32634123
    4. Ishigaki H, Minami T, et al. "EphA2 inhibition suppresses proliferation of small-cell lung cancer cells through inducing cell cycle arrest." Biochem Biophys Res Commun. 2019 Sep 24. pii: S0006-291X(19)31803-0. PMID:31558317
    5. Xi Y, Kim T, et al. "Local lung hypoxia determines epithelial fate decisions during alveolar regeneration." Nat Cell Biol.2017 Aug;19(8):904-914. PMID:28737769

ALW-II-41-27

ALW-II-41-27

Background

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