BI-2563 is a small molecule compound with potential antineoplastic activities. BI 2536 binds to and inhibits Polo-like kinase 1 (Plk1), resulting in mitotic arrest, disruption of cytokinesis, and apoptosis in susceptible tumor cell populations. Plk1, a serine/threonine-protein kinase, is a key regulator of multiple processes fundamental to mitosis and cell division.
1: Müller-Tidow C, Bug G, Lübbert M, Krämer A, Krauter J, Valent P, Nachbaur D, Berdel WE, Ottmann OG, Fritsch H, Munzert G, Garin-Chesa P, Fleischer F, Taube T, Döhner H. A randomized, open-label, phase I/II trial to investigate the maximum tolerated dose of the Polo-like kinase inhibitor BI 2536 in elderly patients with refractory/relapsed acute myeloid leukaemia. Br J Haematol. 2013 Oct;163(2):214-22. doi: 10.1111/bjh.12518. Epub 2013 Aug 16. PubMed PMID: 24033250.
2: Wu CP, Hsiao SH, Sim HM, Luo SY, Tuo WC, Cheng HW, Li YQ, Huang YH, Ambudkar SV. Human ABCB1 (P-glycoprotein) and ABCG2 mediate resistance to BI 2536, a potent and selective inhibitor of Polo-like kinase 1. Biochem Pharmacol. 2013 Oct 1;86(7):904-13. doi: 10.1016/j.bcp.2013.08.004. Epub 2013 Aug 17. PubMed PMID: 23962445; PubMed Central PMCID: PMC3791609.
3: Vose JM, Friedberg JW, Waller EK, Cheson BD, Juvvigunta V, Fritsch H, Petit C, Munzert G, Younes A. The Plk1 inhibitor BI 2536 in patients with refractory or relapsed non-Hodgkin lymphoma: a phase I, open-label, single dose-escalation study. Leuk Lymphoma. 2013 Apr;54(4):708-13. doi: 10.3109/10428194.2012.729833. Epub 2012 Oct 4. PubMed PMID: 22978685.
4: Haupenthal J, Bihrer V, Korkusuz H, Kollmar O, Schmithals C, Kriener S, Engels K, Pleli T, Benz A, Canamero M, Longerich T, Kronenberger B, Richter S, Waidmann O, Vogl TJ, Zeuzem S, Piiper A. Reduced efficacy of the Plk1 inhibitor BI 2536 on the progression of hepatocellular carcinoma due to low intratumoral drug levels. Neoplasia. 2012 May;14(5):410-9. PubMed PMID: 22745587; PubMed Central PMCID: PMC3384428.
5: Mross K, Dittrich C, Aulitzky WE, Strumberg D, Schutte J, Schmid RM, Hollerbach S, Merger M, Munzert G, Fleischer F, Scheulen ME. A randomised phase II trial of the Polo-like kinase inhibitor BI 2536 in chemo-naïve patients with unresectable exocrine adenocarcinoma of the pancreas - a study within the Central European Society Anticancer Drug Research (CESAR) collaborative network. Br J Cancer. 2012 Jul 10;107(2):280-6. doi: 10.1038/bjc.2012.257. Epub 2012 Jun 14. PubMed PMID: 22699824; PubMed Central PMCID: PMC3394983.
6: Ellis PM, Chu QS, Leighl N, Laurie SA, Fritsch H, Gaschler-Markefski B, Gyorffy S, Munzert G. A phase I open-label dose-escalation study of intravenous BI 2536 together with pemetrexed in previously treated patients with non-small-cell lung cancer. Clin Lung Cancer. 2013 Jan;14(1):19-27. doi: 10.1016/j.cllc.2012.04.003. Epub 2012 Jun 1. PubMed PMID: 22658814.
7: de Oliveira JC, Brassesco MS, Pezuk JA, Morales AG, Valera ET, Montaldi AP, Sakamoto-Hojo ET, Scrideli CA, Tone LG. In vitro PLK1 inhibition by BI 2536 decreases proliferation and induces cell-cycle arrest in melanoma cells. J Drugs Dermatol. 2012 May;11(5):587-92. PubMed PMID: 22527426.
8: Frost A, Mross K, Steinbild S, Hedbom S, Unger C, Kaiser R, Trommeshauser D, Munzert G. Phase i study of the Plk1 inhibitor BI 2536 administered intravenously on three consecutive days in advanced solid tumours. Curr Oncol. 2012 Feb;19(1):e28-35. doi: 10.3747/co.19.866. PubMed PMID: 22328845; PubMed Central PMCID: PMC3267594.
9: Pezuk JA, Brassesco MS, Oliveira JC, Morales AG, Montaldi AP, Sakamoto-Hojo ET, Scrideli CA, Tone LG. Antiproliferative in vitro effects of BI 2536-mediated PLK1 inhibition on cervical adenocarcinoma cells. Clin Exp Med. 2013 Feb;13(1):75-80. doi: 10.1007/s10238-011-0166-1. Epub 2011 Nov 12. PubMed PMID: 22080235.
10: Morales AG, Brassesco MS, Pezuk JA, Oliveira JC, Montaldi AP, Sakamoto-Hojo ET, Scrideli CA, Tone LG. BI 2536-mediated PLK1 inhibition suppresses HOS and MG-63 osteosarcoma cell line growth and clonogenicity. Anticancer Drugs. 2011 Nov;22(10):995-1001. doi: 10.1097/CAD.0b013e32834a16d4. PubMed PMID: 21822121.
Chemical |
CAS Num |
755038-02-9 |
Chemical Formula |
C28H39N7O3 |
Molecular Weight |
521.65 |
IUPAC Chemical Name |
(R)-4-((8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl)amino)-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide |
Exact Mass |
521.31144 |
Elemental Analysis |
C, 64.47; H, 7.54; N, 18.80; O, 9.20 |
Synonym |
BI2536; BI-2536 BI 2536. |
Solubility |
Soluble in DMSO, not in water |
SMILES Code |
O=C(NC1CCN(C)CC1)C2=CC=C(NC(N=C3N(C4CCCC4)[C@@H]5CC)=NC=C3N(C)C5=O)C(OC)=C2 |
Biological |
Targets and Effects |
N/A |
Pathways |
Apoptosis |
Physical |
Appearance |
Off-white to yellow solid powder |
Purity |
>98% (or refer to the Certificate of Analysis) |
Shipping Condition |
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
Storage Condition |
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
Shelf Life |
>2 years if stored properly |