化学名称 : HMN-214(IVX-214)/HMN214
CAS : 173529-46-9
溶解度:Soluble in DMSO
储存条件:-20C 2 years
BI 2536 is a small molecule compound with potential antineoplastic activities. BI 2536 binds to and inhibits Polo-like kinase 1 (Plk1, derived from human, mouse and rat) (with IC50of 0.83 nM), resulting in mitotic arrest, disruption of cytokinesis, and apoptosis in susceptible tumor cell populations.This compound showed a more than 1000-fold selectivity relative to a panel of 63 other protein kinases, but it also affected the activities of Plk2 at an IC50 of 3.5 nM and, to a slightly lesser extent, the activity of Plk3 (IC50 9.0 nM).BI 2536 inhibits growth of human tumor xenografts in nude mice and induces regression of large tumors with well-tolerated intravenous dose regimens.
1. Steegmaier M, Hoffmann M, Baum A, L��n��rt P, Petronczki M, Krss��k M, G��rtler U, Garin-Chesa P, Lieb S, Quant J, Grauert M, Adolf GR, Kraut N, Peters JM, Rettig WJ. BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo. Curr Biol. 2007 Feb 20;17(4):316-22. Epub 2007 Feb 8. 2. L��n��rt P, Petronczki M, Steegmaier M, Di Fiore B, Lipp JJ, Hoffmann M, Rettig WJ, Kraut N, Peters JM. The small-molecule inhibitor BI 2536 reveals novel insights into mitotic roles of polo-like kinase 1. Curr Biol. 2007 Feb 20;17(4):304-15. Epub 2007 Feb 8. 3. Mross K, Frost A, Steinbild S, Hedbom S, Rentschler J, Kaiser R, Rouyrre N, Trommeshauser D, Hoesl CE, Munzert G. Phase I dose escalation and pharmacokinetic study of BI 2536, a novel Polo-like kinase 1 inhibitor, in patients with advanced solid tumors. J Clin Oncol. 2008 Dec 1;26(34):5511-7. Epub 2008 Oct 27.