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ALW-II-41-27

Cat. No. M8974
ALW-II-41-27 Structure
Size Price Availability Quantity
5mg USD 355 In stock
10mg USD 465 In stock
50mg USD 1240 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Protocol
Cell Experiment
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.
Concentrations 1 μM
Incubation time 72 h
Animal Experiment
Animal models 6-week-old athymic nude mice
Formulation
Dosages 15, 30 mg/kg, twice daily
Administration Intraperitoneal injection
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 607.69
Formula C32H32F3N5O2S
CAS Number 1186206-79-0
Purity >98%
Solubility DMSO: ≥ 30 mg/mL
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ALW-II-41-27 supplier, inhibitors

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