Volasertib（Cat No.:I004793）, also known as BI 6727, is a highly potent inhibitor of Polo-like kinase 1 (Plk1). It exhibits an impressive IC50 value of 0.87 nM in cell-free assays, indicating its strong inhibitory activity against Plk1. Notably, it displays significantly higher selectivity for Plk1 compared to Plk2 and Plk3, with 6- and 65-fold selectivity, respectively. Volasertib has shown the ability to induce cell cycle arrest and stimulate autophagy in various cancer cells. These properties make it a promising candidate for cancer treatment and an important tool for studying Plk1-related cellular processes.
| Catalog Number | I004793 |
| CAS Number | 755038-65-4 |
| Synonyms | N-[4-[4-(cyclopropylmethyl)piperazin-1-yl]cyclohexyl]-4-[[(7R)-7-ethyl-5-methyl-6-oxo-8-propan-2-yl-7H-pteridin-2-yl]amino]-3-methoxybenzamide |
| Molecular Formula | C₃₄H₅₀N₈O₃ |
| Purity | ≥95% |
| Target | PLK |
| Solubility | DMSO ≥22mg/mL Water <1.2mg/mL Ethanol ≥122mg/mL |
| Storage | -20°C |
| IC50 | 0.87 nM |
| IUPAC Name | N-[4-[4-(cyclopropylmethyl)piperazin-1-yl]cyclohexyl]-4-[[(7R)-7-ethyl-5-methyl-6-oxo-8-propan-2-yl-7H-pteridin-2-yl]amino]-3-methoxybenzamide |
| InChI | InChI=1S/C34H50N8O3/c1-6-28-33(44)39(4)29-20-35-34(38-31(29)42(28)22(2)3)37-27-14-9-24(19-30(27)45-5)32(43)36-25-10-12-26(13-11-25)41-17-15-40(16-18-41)21-23-7-8-23/h9,14,19-20,22-23,25-26,28H,6-8,10-13,15-18,21H2,1-5H3,(H,36,43)(H,35,37,38)/t25?,26?,28-/m1/s1 |
| InChIKey | SXNJFOWDRLKDSF-XKHVUIRMSA-N |
| SMILES | CCC1C(=O)N(C2=CN=C(N=C2N1C(C)C)NC3=C(C=C(C=C3)C(=O)NC4CCC(CC4)N5CCN(CC5)CC6CC6)OC)C |
| Reference | </br>1:Pre-clinical drug screen reveals topotecan, actinomycin D and volasertib as potential new therapeutic candidates for ETMR brain tumor patients. Schmidt C, Schubert NA, Brabetz S, Mack N, Schwalm B, Chan JA, Selt F, Herold-Mende C, Witt O, Milde T, Pfister SM, Korshunov A, Kool M.Neuro Oncol. 2017 May 8. doi: 10.1093/neuonc/nox093. [Epub ahead of print] PMID: 28482026 </br>2:Proteasome inhibition enhances the efficacy of volasertib-induced mitotic arrest in AML in vitro and prolongs survival in vivo. Schnerch D, Schüler J, Follo M, Felthaus J, Wider D, Klingner K, Greil C, Duyster J, Engelhardt M, Wäsch R.Oncotarget. 2017 Mar 28;8(13):21153-21166. doi: 10.18632/oncotarget.15503. PMID: 28416751 Free PMC Article</br>3:Volasertib suppresses the growth of human hepatocellular carcinoma <i>in vitro</i> and <i>in vivo</i>. Zheng DW, Xue YQ, Li Y, Di JM, Qiu JG, Zhang WJ, Jiang QW, Yang Y, Chen Y, Wei MN, Huang JR, Wang K, Wei X, Shi Z.Am J Cancer Res. 2016 Nov 1;6(11):2476-2488. eCollection 2016. PMID: 27904765 Free PMC Article</br>4:Small molecule inhibition of polo-like kinase 1 by volasertib (BI 6727) causes significant melanoma growth delay and regression in vivo. Cholewa BD, Ndiaye MA, Huang W, Liu X, Ahmad N.Cancer Lett. 2017 Jan 28;385:179-187. doi: 10.1016/j.canlet.2016.10.025. Epub 2016 Oct 25. PMID: 27793694 </br>5:Spotlight on Volasertib: Preclinical and Clinical Evaluation of a Promising Plk1 Inhibitor. Van den Bossche J, Lardon F, Deschoolmeester V, De Pauw I, Vermorken JB, Specenier P, Pauwels P, Peeters M, Wouters A.Med Res Rev. 2016 Jul;36(4):749-86. doi: 10.1002/med.21392. Epub 2016 May 3. Review. PMID: 27140825 </br>6:Volasertib suppresses tumor growth and potentiates the activity of cisplatin in cervical cancer. Xie FF, Pan SS, Ou RY, Zheng ZZ, Huang XX, Jian MT, Qiu JG, Zhang WJ, Jiang QW, Yang Y, Li WF, Shi Z, Yan XJ.Am J Cancer Res. 2015 Nov 15;5(12):3548-59. eCollection 2015. PMID: 26885445 Free PMC Article</br>7:Polo-like Kinase Inhibitor Volasertib Exhibits Antitumor Activity and Synergy with Vincristine in Pediatric Malignancies. Abbou S, Lanvers-Kaminsky C, Daudigeos-Dubus E, LE Dret L, Laplace-Builhe C, Molenaar J, Vassal G, Geoerger B; within the ITCC Biology and Preclinical Evaluation Committee..Anticancer Res. 2016 Feb;36(2):599-609. PMID: 26851014 </br>8:Volasertib Versus Chemotherapy in Platinum-Resistant or -Refractory Ovarian Cancer: A Randomized Phase II Groupe des Investigateurs Nationaux pour l/’Etude des Cancers de l/’Ovaire Study. Pujade-Lauraine E, Selle F, Weber B, Ray-Coquard IL, Vergote I, Sufliarsky J, Del Campo JM, Lortholary A, Lesoin A, Follana P, Freyer G, Pardo B, Vidal L, Tholander B, Gladieff L, Sassi M, Garin-Chesa P, Nazabadioko S, Marzin K, Pilz K, Joly F.J Clin Oncol. 2016 Mar 1;34(7):706-13. doi: 10.1200/JCO.2015.62.1474. Epub 2016 Jan 11. PMID: 26755507 </br>9:Phase I trial of volasertib, a Polo-like kinase inhibitor, in Japanese patients with advanced solid tumors. Nokihara H, Yamada Y, Fujiwara Y, Yamamoto N, Wakui H, Nakamichi S, Kitazono S, Inoue K, Harada A, Taube T, Takeuchi Y, Tamura T.Invest New Drugs. 2016 Feb;34(1):66-74. doi: 10.1007/s10637-015-0300-0. Epub 2015 Dec 2. PMID: 26627079 </br>10:Phase I trial of volasertib, a Polo-like kinase inhibitor, in Japanese patients with acute myeloid leukemia. Kobayashi Y, Yamauchi T, Kiyoi H, Sakura T, Hata T, Ando K, Watabe A, Harada A, Taube T, Miyazaki Y, Naoe T.Cancer Sci. 2015 Nov;106(11):1590-5. doi: 10.1111/cas.12814. Epub 2015 Oct 21. PMID: 26471242 Free PMC Article |
