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1453176-83-4

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1453176-83-4 Usage

Check Digit Verification of cas no

The CAS Registry Mumber 1453176-83-4 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,4,5,3,1,7 and 6 respectively; the second part has 2 digits, 8 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 1453176-83:
(9*1)+(8*4)+(7*5)+(6*3)+(5*1)+(4*7)+(3*6)+(2*8)+(1*3)=164
164 % 10 = 4
So 1453176-83-4 is a valid CAS Registry Number.

1453176-83-4Relevant articles and documents

Identification of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with no evidence of CYP3A4 time-dependent inhibition and improved aqueous solubility

Zak, Mark,Liederer, Bianca M.,Sampath, Deepak,Yuen, Po-Wai,Bair, Kenneth W.,Baumeister, Timm,Buckmelter, Alexandre J.,Clodfelter, Karl H.,Cheng, Eric,Crocker, Lisa,Fu, Bang,Han, Bingsong,Li, Guangkun,Ho, Yen-Ching,Lin, Jian,Liu, Xiongcai,Ly, Justin,O'Brien, Thomas,Reynolds, Dominic J.,Skelton, Nicholas,Smith, Chase C.,Tay, Suzanne,Wang, Weiru,Wang, Zhongguo,Xiao, Yang,Zhang, Lei,Zhao, Guiling,Zheng, Xiaozhang,Dragovich, Peter S.

, p. 529 - 541 (2015/03/05)

Herein we report the optimization efforts to ameliorate the potent CYP3A4 time-dependent inhibition (TDI) and low aqueous solubility exhibited by a previously identified lead compound from our NAMPT inhibitor program (1, GNE-617). Metabolite identification studies pinpointed the imidazopyridine moiety present in 1 as the likely source of the TDI signal, and replacement with other bicyclic systems was found to reduce or eliminate the TDI finding. A strategy of reducing the number of aromatic rings and/or lowering c Log D7.4 was then employed to significantly improve aqueous solubility. These efforts culminated in the discovery of 42, a compound with no evidence of TDI, improved aqueous solubility, and robust efficacy in tumor xenograft studies.

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