For research use only. Not for therapeutic Use.
BI-2536（Cat No.:I004792）is a potent and selective inhibitor of polo-like kinase 1 (PLK1), a critical regulator of cell division and mitotic progression. By inhibiting PLK1, BI-2536 disrupts the normal cell cycle, leading to cell cycle arrest and apoptosis in cancer cells. This compound has demonstrated significant anticancer activity in preclinical studies across various malignancies, including solid tumors and hematologic cancers. Its targeted action allows for the potential reduction of side effects commonly associated with traditional chemotherapies. Ongoing clinical trials are investigating BI-2536’s efficacy and safety, aiming to position it as a valuable therapeutic option in oncology.
| Catalog Number | I004792 |
| CAS Number | 755038-02-9 |
| Synonyms | 4-[[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide |
| Molecular Formula | C₂₈H₃₉N₇O₃ |
| Purity | ≥95% |
| Target | PLK |
| Solubility | DMSO ≥100mg/mL Water <1.2mg/mL Ethanol ≥100mg/mL |
| Storage | 3 years -20C powder |
| IC50 | 0.83 nM (Plk1); 25 nM (BRD4) |
| IUPAC Name | 4-[[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide |
| InChI | InChI=1S/C28H39N7O3/c1-5-22-27(37)34(3)23-17-29-28(32-25(23)35(22)20-8-6-7-9-20)31-21-11-10-18(16-24(21)38-4)26(36)30-19-12-14-33(2)15-13-19/h10-11,16-17,19-20,22H,5-9,12-15H2,1-4H3,(H,30,36)(H,29,31,32)/t22-/m1/s1 |
| InChIKey | XQVVPGYIWAGRNI-JOCHJYFZSA-N |
| SMILES | CC[C@@H]1C(=O)N(C2=CN=C(N=C2N1C3CCCC3)NC4=C(C=C(C=C4)C(=O)NC5CCN(CC5)C)OC)C |
| Reference | </br>1:An open-label, phase II study of the polo-like kinase-1 (Plk-1) inhibitor, BI 2536, in patients with relapsed small cell lung cancer (SCLC). Awad MM, Chu QS, Gandhi L, Stephenson JJ, Govindan R, Bradford DS, Bonomi PD, Ellison DM, Eaton KD, Fritsch H, Munzert G, Johnson BE, Socinski MA.Lung Cancer. 2017 Feb;104:126-130. doi: 10.1016/j.lungcan.2016.12.019. Epub 2016 Dec 30. PMID: 28212994 </br>2:BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536. Chen L, Yap JL, Yoshioka M, Lanning ME, Fountain RN, Raje M, Scheenstra JA, Strovel JW, Fletcher S.ACS Med Chem Lett. 2015 May 18;6(7):764-9. doi: 10.1021/acsmedchemlett.5b00084. eCollection 2015 Jul 9. PMID: 26191363 Free PMC Article</br>3:Pharmacological inhibition of Polo-like kinase 1 (PLK1) by BI-2536 decreases the viability and survival of hamartin and tuberin deficient cells via induction of apoptosis and attenuation of autophagy. Valianou M, Cox AM, Pichette B, Hartley S, Paladhi UR, Astrinidis A.Cell Cycle. 2015;14(3):399-407. doi: 10.4161/15384101.2014.986394. PMID: 25565629 Free PMC Article</br>4:PLK1 expression and BI 2536 effects in childhood acute lymphoblastic leukemia. Oliveira JC, Pezuk JA, Brassesco MS, Morales AG, Queiroz RG, Scrideli CA, Tone LG.Pediatr Blood Cancer. 2014 Jul;61(7):1227-31. doi: 10.1002/pbc.24978. Epub 2014 Feb 12. PMID: 24519995 </br>5: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. 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.Br J Haematol. 2013 Oct;163(2):214-22. doi: 10.1111/bjh.12518. Epub 2013 Aug 16. PMID: 24033250 </br>6:Human ABCB1 (P-glycoprotein) and ABCG2 mediate resistance to BI 2536, a potent and selective inhibitor of Polo-like kinase 1. Wu CP, Hsiao SH, Sim HM, Luo SY, Tuo WC, Cheng HW, Li YQ, Huang YH, Ambudkar SV.Biochem Pharmacol. 2013 Oct 1;86(7):904-13. doi: 10.1016/j.bcp.2013.08.004. Epub 2013 Aug 17. PMID: 23962445 Free PMC Article</br>7:The Plk1 inhibitor BI 2536 in patients with refractory or relapsed non-Hodgkin lymphoma: a phase I, open-label, single dose-escalation study. Vose JM, Friedberg JW, Waller EK, Cheson BD, Juvvigunta V, Fritsch H, Petit C, Munzert G, Younes A.Leuk Lymphoma. 2013 Apr;54(4):708-13. doi: 10.3109/10428194.2012.729833. Epub 2012 Oct 4. PMID: 22978685 </br>8:Reduced efficacy of the Plk1 inhibitor BI 2536 on the progression of hepatocellular carcinoma due to low intratumoral drug levels. 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.Neoplasia. 2012 May;14(5):410-9. PMID: 22745587 Free PMC Article</br>9: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. Mross K, Dittrich C, Aulitzky WE, Strumberg D, Schutte J, Schmid RM, Hollerbach S, Merger M, Munzert G, Fleischer F, Scheulen ME.Br J Cancer. 2012 Jul 10;107(2):280-6. doi: 10.1038/bjc.2012.257. Epub 2012 Jun 14. PMID: 22699824 Free PMC Article</br>10: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. Ellis PM, Chu QS, Leighl N, Laurie SA, Fritsch H, Gaschler-Markefski B, Gyorffy S, Munzert G.Clin Lung Cancer. 2013 Jan;14(1):19-27. doi: 10.1016/j.cllc.2012.04.003. Epub 2012 Jun 1. PMID: 22658814 |
