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1186206-79-0

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1186206-79-0 Usage

Biological Activity

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].

references

[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.

Check Digit Verification of cas no

The CAS Registry Mumber 1186206-79-0 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,1,8,6,2,0 and 6 respectively; the second part has 2 digits, 7 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 1186206-79:
(9*1)+(8*1)+(7*8)+(6*6)+(5*2)+(4*0)+(3*6)+(2*7)+(1*9)=160
160 % 10 = 0
So 1186206-79-0 is a valid CAS Registry Number.

1186206-79-0SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 17, 2017

Revision Date: Aug 17, 2017

1.Identification

1.1 GHS Product identifier

Product name N-[5-[[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]carbamoyl]-2-methylphenyl]-5-thiophen-2-ylpyridine-3-carboxamide

1.2 Other means of identification

Product number -
Other names HMS2043H01

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:1186206-79-0 SDS

1186206-79-0Downstream Products

1186206-79-0Relevant articles and documents

A Putative Single-Photon Emission CT Imaging Tracer for Erythropoietin-Producing Hepatocellular A2 Receptor

Arimitsu, Kenji,Furukawa, Takenori,Kawashima, Hidekazu,Kimura, Hiroyuki,Torimoto, Hanae,Yagi, Yusuke,Yasui, Hiroyuki

, p. 1238 - 1244 (2021/08/01)

Erythropoietin-producing hepatocellular (Eph) receptors are receptor tyrosine kinases involved in cell-cell contact. The EphA2 receptor is associated with cancer proliferation and migration. Therefore, EphA2 receptor imaging has the potential for cancer d

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