SP-146 is a highly potent, selective and non-ATP-competitive Aurora B inhibitor with an IC50 of 0.316 nM, and shows >2000 fold selectivity against FLT3 (IC50=1475.6 nM) and KIT (IC50=1307.6 nM). SP-146 is not promiscuous, rather selective for a few cancer cells, incluing MDA-MD-468 (GI50=107 nM). SP-146 can be used for the research of triple negative breast cancer (TNBC).
SP-146 (0-1 µM; 24 hours) is not promiscuous, rather selective for a few cell lines, it inhibits MDA-MB-468, CCRF-CEM, COLO 205 and A498 cell growth with GI50 values of 107 nM,47.4 nM, 50.3 nM and 53.2 nM, respectively[1].
SP-146 (63.2 nM) inhibits Aurora B activity in H460 cells by the characteristics of increased DNA content, and it increases cell volume with enormous nucleus[1].
SP-146 (0-2 µM) inhibits Aurora B enzymatic activity with an IC50 of 0.316 nM and inhibits Aurora A with observed IC50 value of 18.975 nM. SP-146 shows >2000 fold selectivity against FLT3 (IC50=1475.6 nM) and KIT (IC50=1307.6 nM). Meanwhile, it exhibits inhibitory effects on other receptor tyrosine kinases (RTKs) namely EGFR, RET and HER2 with IC50 value ≥2 µM[1].
Reference:
[1]. Naga Rajiv Lakkaniga,et al. Discovery of SP-96, the first non-ATP-competitive Aurora Kinase B inhibitor, for reduced myelosuppression.Eur J Med Chem. 2020 Jul 12;203:112589.