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1362154-70-8

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1362154-70-8 Usage

General Description

GNE 617 is a potent and selective inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR) tyrosine kinases. It has been found to inhibit the growth and survival of various cancer cell lines and has shown promising anti-tumor activity in preclinical studies. GNE 617 has also been shown to sensitize cancer cells to chemotherapy and radiation therapy, making it a potential candidate for combination therapy in the treatment of solid tumors. Its ability to specifically target the IGF-1R and IR pathways makes it a valuable tool for understanding the role of these receptors in cancer progression and for developing targeted therapies for cancer treatment.

Check Digit Verification of cas no

The CAS Registry Mumber 1362154-70-8 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,3,6,2,1,5 and 4 respectively; the second part has 2 digits, 7 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 1362154-70:
(9*1)+(8*3)+(7*6)+(6*2)+(5*1)+(4*5)+(3*4)+(2*7)+(1*0)=138
138 % 10 = 8
So 1362154-70-8 is a valid CAS Registry Number.

1362154-70-8Downstream Products

1362154-70-8Relevant articles and documents

Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (Nampt) inhibitors

Zheng, Xiaozhang,Bauer, Paul,Baumeister, Timm,Buckmelter, Alexandre J.,Caligiuri, Maureen,Clodfelter, Karl H.,Han, Bingsong,Ho, Yen-Ching,Kley, Nikolai,Lin, Jian,Reynolds, Dominic J.,Sharma, Geeta,Smith, Chase C.,Wang, Zhongguo,Dragovich, Peter S.,Gunzner-Toste, Janet,Liederer, Bianca M.,Ly, Justin,O'Brien, Thomas,Oh, Angela,Wang, Leslie,Wang, Weiru,Xiao, Yang,Zak, Mark,Zhao, Guiling,Yuen, Po-Wai,Bair, Kenneth W.

, p. 6413 - 6433 (2013/09/23)

Crystal structures of several urea- and thiourea-derived compounds in complex with the nicotinamide phosphoribosyltransferase (Nampt) protein were utilized to design a potent amide-containing inhibitor bearing an aza-indole moiety (7, Nampt BC IC50 = 9.0 nM, A2780 cell proliferation IC 50 = 10 nM). The Nampt-7 cocrystal structure was subsequently obtained and enabled the design of additional amide-containing inhibitors which incorporated various other fused 6,5-heterocyclic moieties and biaryl sulfone or sulfonamide motifs. Additional modifications of these molecules afforded many potent biaryl sulfone-containing Nampt inhibitors which also exhibited favorable in vitro ADME properties (microsomal and hepatocyte stability, MDCK permeability, plasma protein binding). An optimized compound (58) was a potent inhibitor of multiple cancer cell lines (IC50 10 nM vs U251, HT1080, PC3, MiaPaCa2, and HCT116 lines), displayed acceptable mouse PK properties (F = 41%, CL = 52.4 mL/min/kg), and exhibited robust efficacy in a U251 mouse xenograft model.

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