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ALW-II-41-27
Cat No.
CEI-1209
Product Overview
ALW-II-41-27 is a potent inhibitor of EPH family kinases, with an IC50 value of 11 nM to EPHA2.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.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.
CAS No.
1186206-79-0
Molecular Weight
607.69
Storage
Store at -20°C
Synonyms
Eph receptor tyrosine kinase inhibitor;
Targets
Eph receptor
Chemical Name
N-[5-[[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]carbamoyl]-2-methylphenyl]-5-thiophen-2-ylpyridine-3-carboxamide
Solubility
DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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