SCH-1473759

• CAT Number: I000398
• CAS Number: 1094069-99-4
• Molecular Formula: C20H26N8OS
• Molecular Weight: 426.54
• Purity: ≥95%
• 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
• Target: Aurora Kinase
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 4 nM (Aurora A); 13 nM (Aurora B)[1].
• InChI: InChI=1S/C20H26N8OS/c1-5-27(20(3,4)12-29)11-15-6-17(30-26-15)25-18-19-21-9-16(14-7-22-23-8-14)28(19)10-13(2)24-18/h6-10,29H,5,11-12H2,1-4H3,(H,22,23)(H,24,25)
• InChIKey: RHGZQGXELRMGES-UHFFFAOYSA-N
• SMILES: CCN(CC1=NSC(=C1)NC2=NC(=CN3C2=NC=C3C4=CNN=C4)C)C(C)(C)CO

SCH 1473759 (Cat.No:I000398) 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). 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.

Reference

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