GSK-923295

• CAT Number: I000375
• CAS Number: 1088965-37-0
• Molecular Formula: C32H38ClN5O4
• Molecular Weight: 592.10
• Purity: ≥95%
• Synonyms: 3-chloro-N-[(2S)-1-[[2-(dimethylamino)acetyl]amino]-3-[4-[8-[(1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl]phenyl]propan-2-yl]-4-propan-2-yloxybenzamide
• Target: Kinesin
• Solubility: in DMSO > 10 mM
• Storage: Store at -20°C
• IC50: 3.2 nM(Ki)
• InChI: InChI=1S/C32H38ClN5O4/c1-20(2)42-29-13-12-24(16-27(29)33)32(41)35-25(17-34-30(40)19-37(4)5)15-22-8-10-23(11-9-22)28-18-38-14-6-7-26(21(3)39)31(38)36-28/h6-14,16,18,20-21,25,39H,15,17,19H2,1-5H3,(H,34,40)(H,35,41)/t21-,25-/m0/s1
• InChIKey: WHMXDBPHBVLYRC-OFVILXPXSA-N
• SMILES: C[C@@H](C1=CC=CN2C1=NC(=C2)C3=CC=C(C=C3)C[C@@H](CNC(=O)CN(C)C)NC(=O)C4=CC(=C(C=C4)OC(C)C)Cl)O

GSK-923295（Cat No.:I000375）is a selective inhibitor of the protein kinase Aurora A, which plays a critical role in cell division and mitotic processes. By inhibiting Aurora A, GSK-923295 disrupts the proper alignment and segregation of chromosomes during mitosis, leading to the inhibition of cancer cell proliferation. It has shown promising results in preclinical studies against various cancers, including solid tumors and hematologic malignancies. The compound is under investigation in clinical trials to evaluate its safety, efficacy, and potential as a targeted therapy, particularly in cancers with overexpressed Aurora A.

Reference

[1]. Xiangping Qian et al Discovery of the First Potent and Selective Inhibitor of Centromere-Associated Protein E: GSK923295. ACS Med. Chem. Lett., 2010, 1 (1), pp 30-34
[2]. Chung V, Heath EI, Schelman WR, Johnson BM, Kirby LC, Lynch KM, Botbyl JD, Lampkin TA, Holen KD.First-time-in-human study of GSK923295, a novel antimitotic inhibitor of centromere-associated protein E (CENP-E), in patients with refractory cancer.Cancer Chemother Pharmacol. 2012 Mar;69(3):733-41. Epub 2011 Oct 22.
[3]. Mayes PA, Degenhardt YY, Wood A, Toporovskya Y, Diskin SJ, Haglund E, Moy C, Wooster R, Maris JM.Mitogen-activated protein kinase (MEK/ERK) inhibition sensitizes cancer cells to centromere-associated protein E (CENP-E) inhibition.Int J Cancer. 2012 Sep 5.
[4]. Balamuth NJ, Wood A, Wang Q, Jagannathan J, Mayes P, Zhang Z, Chen Z, Rappaport E, Courtright J, Pawel B, Weber B, Wooster R, Sekyere EO, Marshall GM, Maris JM.Serial transcriptome analysis and cross-species integration identifies centromere-associated protein E as a novel neuroblastoma target.Cancer Res. 2010 Apr 1;70(7):2749-58. Epub 2010 Mar 16.
[5]. Wood KW, Lad L, Luo L, Qian X, Knight SD, Nevins N, Brejc K, Sutton D, Gilmartin AG, Chua PR, Desai R, Schauer SP, McNulty DE, Annan RS, Belmont LD, Garcia C, Lee Y, Diamond MA, Faucette LF, Giardiniere M, Zhang S, Sun CM, Vidal JD, Lichtsteiner S, Cornwell WD, Greshock JD, Wooster RF, Finer JT, Copeland RA, Huang PS, Morgans DJ Jr, Dhanak D, Bergnes G, Sakowicz R, Jackson JR.Antitumor activity of an allosteric inhibitor of centromere-associated protein-E.Proc Natl Acad Sci U S A. 2010 Mar 30;107(13):5839-44. Epub 2010 Feb 18.