GSK-1070916

• CAT Number: I005606
• CAS Number: 942918-07-2
• Molecular Formula: C₃₀H₃₃N₇O
• Molecular Weight: 507.63
• Purity: ≥95%
• Target: Aurora Kinase
• Solubility: DMSO 101 mg/mL; Water <1 mg/mL
• Storage: Store at -20°C
• IC50: 3.5 nM(Aurora B); 6.5 nM(Aurora C)
• IUPAC Name: 3-[4-[4-[2-[3-[(dimethylamino)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-ethylpyrazol-3-yl]phenyl]-1,1-dimethylurea
• InChI: InChI=1S/C30H33N7O/c1-6-37-19-26(28(34-37)21-10-12-23(13-11-21)32-30(38)36(4)5)24-14-15-31-29-25(24)17-27(33-29)22-9-7-8-20(16-22)18-35(2)3/h7-17,19H,6,18H2,1-5H3,(H,31,33)(H,32,38)
• InChIKey: QTBWCSQGBMPECM-UHFFFAOYSA-N
• SMILES: CCN1C=C(C(=N1)C2=CC=C(C=C2)NC(=O)N(C)C)C3=C4C=C(NC4=NC=C3)C5=CC=CC(=C5)CN(C)C

GSK1070916（Cat No.:I005606）is a potent inhibitor of Aurora B/C, enzymes involved in cell division and mitosis. It selectively targets Aurora B/C, with IC50 values of 3.5 nM and 6.5 nM, respectively. It demonstrates high selectivity for Aurora B/C over Aurora A, particularly when bound to TPX2. By competitively binding to the ATP-binding site, GSK1070916 interferes with the activity of Aurora B/C, potentially leading to cell cycle arrest and inhibition of tumor cell growth. It holds promise as a targeted therapy in cancer treatment.

Reference

[1]. Anderson K, et al. Biochemical characterization of GSK1070916, a potent and selective inhibitor of Aurora B and Aurora C kinases with an extremely long residence time1. Biochem J. 2009 May 13;420(2):259-65.
Abstract 


[2]. Hardwicke, Mary Ann; Oleykowski, Catherine A.; Plant, Ramona; GSK1070916, a potent Aurora B/C kinase inhibitor with broad antitumor activity in tissue culture cells and human tumor xenograft models. Molecular Cancer Therapeutics (2009), 8(7), 1808-1817. 


[3]. Moy C, Oleykowski CA, Plant R, Greshock J, Jing J, Bachman K, Hardwicke MA, Wooster R, Degenhardt Y.High chromosome number in hematological cancer cell lines is a negative predictor of response to the inhibition of Aurora B and C by GSK1070916.J Transl Med. 2011 Jul 15;9:110. 


[4]. Adams ND, Adams JL, Burgess JL, Chaudhari AM, Copeland RA, Donatelli CA, Drewry DH, Fisher KE, Hamajima T, Hardwicke MA, Huffman WF, Koretke-Brown KK, Lai ZV, McDonald OB, Nakamura H, Newlander KA, Oleykowski CA, Parrish CA, Patrick DR, Plant R, Sarpong MA, Sasaki K, Schmidt SJ, Silva DJ, Sutton D, Tang J, Thompson CS, Tummino PJ, Wang JC, Xiang H, Yang J, Dhanak D.Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.J Med Chem. 2010 May 27;53(10):3973-4001. 


[5]. Medina JR, Grant SW, Axten JM, Miller WH, Donatelli CA, Hardwicke MA, Oleykowski CA, Liao Q, Plant R, Xiang H.Discovery of a new series of Aurora inhibitors through truncation of GSK1070916.Bioorg Med Chem Lett. 2010 Apr 15;20(8):2552-5. Epub 2010 Mar 1.