SCH-1473759


CAS No. : 1094069-99-4

SCH-1473759,1094069-99-4
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000398
Synonyms:2-[ethyl-[[5-[[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]amino]-1,2-thiazol-3-yl]methyl]amino]-2-methylpropan-1-ol
Molecular Formula:C20H26N8OS
Molecular Weight:426.54
Target:Aurora Kinase
IC50:4 nM (Aurora A); 13 nM (Aurora B)[1].
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Appearance:Solid powder
Purity: > 98%
Cat No:I000398
Cas No:1094069-99-4
Product-Name:SCH-1473759

SCH 1473759 is a novel sub-nanomolar Aurora A/B inhibitor with IC50 of 4 nM and 13 nM, respectively.
IC50 Value: 4 nM (Aurora A); 13 nM (Aurora B)[1].
Target: Aurora Kinase
in vitro: Asynchronous cells required 24-h exposure to SCH 1473759 for maximal induction of >4 N DNA content and inhibition of cell growth. However, following taxane- or KSP inhibitor-induced mitotic arrest, less than 4-h exposure induced >4 N DNA content. This finding correlated with the ability of SCH 1473759 to accelerate exit from mitosis in response to taxane- and KSP inhibitor-induced arrest [2].
in vivo: SCH-1473759 showed efficacy and target engagement in A2780 human tumor xenograft model in mouse, and also acceptable pharmacokinetic dosing in dog, monkey and rodents, on target efficacy, as well as a safety profile in dogs[1].
Clinical trial: N/A


1:A simple and rapid UHPLC-MS/MS method for the quantitation of the dual aurora kinase A/B inhibitor SCH-1473759 in murine plasma. Ferraz Nogueira Filho MA, Peer CJ, Nguyen J, McCalla A, Helman L, Figg WD.J Pharm Biomed Anal. 2017 Jan 5;132:223-226. doi: 10.1016/j.jpba.2016.10.003. Epub 2016 Oct 5. PMID: 27768921
2:SCH 1473759, a novel Aurora inhibitor, demonstrates enhanced anti-tumor activity in combination with taxanes and KSP inhibitors. Basso AD, Liu M, Gray K, Tevar S, Lee S, Liang L, Ponery A, Smith EB, Monsma FJ Jr, Yu T, Zhang Y, Kerekes AD, Esposite S, Xiao Y, Tagat JR, Hicklin DJ, Kirschmeier P.Cancer Chemother Pharmacol. 2011 Oct;68(4):923-33. doi: 10.1007/s00280-011-1568-1. Epub 2011 Feb 5. PMID: 21298383
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