ALW-II-41-27 is a Eph receptor tyrosine kinase inhibitor with an IC50 of 11 nM for EPHA2. 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.
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.
|Cell lines||Non–small cell lung cancer (NSCLC) PC-9/ER, PC-9/ERC15, PC-9/ERC16 cell lines|
|Preparation method||Treatment with 1 μM ALW-II-41-27 inhibited cell proliferation and increased apoptosis in erlotinib-resistant NSCLC cell lines. Apoptosis induced by ALW-II-41-27 was accompanied by the increase of cleavage of caspase-3 and PARP as well as decreased expression of antiapoptotic proteins BCL-xL and MCL-1.|
|Incubation time||72 h|
|Animal models||6-week-old athymic nude mice|
|Dosages||15, 30 mg/kg, twice daily|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 30 mg/mL|
Targeting EphA2 impairs cell cycle progression and growth of basal-like/triple-negative breast cancers.
Song W, et al. Oncogene. 2017 Oct 5;36(40):5620-5630. PMID: 28581527.
Identification of Novel Small Molecule Inhibitors of Oncogenic RET Kinase.
Moccia M, et al. PLoS One. 2015 Jun 5;10(6):e0128364. PMID: 26046350.
Genetic and pharmacologic inhibition of EPHA2 promotes apoptosis in NSCLC.
Amato KR, et al. J Clin Invest. 2014 May;124(5):2037-49. PMID: 24713656.
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