Volasertib - CAS 755038-65-4
Catalog number: 755038-65-4
Category: Inhibitor
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Molecular Formula:
C34H50N8O3
Molecular Weight:
618.827
COA:
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Targets:
Polo-like Kinase (PLK)
Description:
BI 6727 (Volasertib) is a small highly potent Polo-like kinase inhibitor (Plk) with an IC50 of 0 .87 nM and EC50 of 11-37 nM on a panel of cancer cell lines, which exhibited significant anti-proliferative in multiple cancer models, including a model of taxane-resistant colorectal cancer. BI 6727 (Volasertib) caused programmed cell death in colon and non-small cell lung cancer cells both in vitro and in vivo.
Purity:
0.98
Appearance:
white solid powder
Synonyms:
Volasertib; BI-6727; BI6727; BI 6727.
MSDS:
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InChIKey:
SXNJFOWDRLKDSF-XKHVUIRMSA-N
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
Canonical 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
Current Developer:
Boehringer Ingelheim.
1.Phase I trial of volasertib, a Polo-like kinase inhibitor, in Japanese patients with acute myeloid leukemia.
Kobayashi Y1, Yamauchi T2, Kiyoi H3, Sakura T4, Hata T5, Ando K6, Watabe A7, Harada A8, Taube T9, Miyazaki Y5, Naoe T10. Cancer Sci. 2015 Nov;106(11):1590-5. doi: 10.1111/cas.12814. Epub 2015 Oct 21.
This phase I trial conducted in Japanese patients with acute myeloid leukemia evaluated the safety, maximum tolerated dose and pharmacokinetics of volasertib (BI 6727), a selective Polo-like kinase inhibitor. The primary endpoints were the maximum tolerated dose of volasertib and the incidence of dose-limiting toxicities. Secondary endpoints were best response and remission duration. Other endpoints included safety and pharmacokinetics. Patients who were ineligible for standard induction therapy or with relapsed or refractory disease received volasertib monotherapy as a 2-h infusion on days 1 and 15 of a 28-day cycle, with dose escalation following a 3 + 3 design. A total of 19 patients were treated with three volasertib doses: 350, 400 and 450 mg. One patient receiving volasertib 450 mg reported a dose-limiting toxicity of grade 4 abnormal liver function test and 450 mg was determined as the maximum tolerated dose. The most frequently reported adverse events were febrile neutropenia (78.
2.Phase I trial of volasertib, a Polo-like kinase inhibitor, in Japanese patients with advanced solid tumors.
Nokihara H1, Yamada Y2, Fujiwara Y3, Yamamoto N3, Wakui H3, Nakamichi S3, Kitazono S3, Inoue K4,5, Harada A4, Taube T6, Takeuchi Y4, Tamura T3,7. Invest New Drugs. 2016 Feb;34(1):66-74. doi: 10.1007/s10637-015-0300-0. Epub 2015 Dec 2.
Purpose This trial evaluated the maximum tolerated dose (MTD), safety, pharmacokinetics, and clinical effects of volasertib, a selective Polo-like kinase inhibitor that induces mitotic arrest and apoptosis, in Japanese patients with advanced solid tumors (NCT01348347; 1230.15). Methods In this phase I, open-label, dose-escalation trial, sequential patient cohorts (3 + 3 dose-escalation design) received volasertib (200-350 mg) as a single dose by intravenous infusion over 2 h on day 1 every 21 days until disease progression or unacceptable toxicity. The primary endpoint was the MTD of volasertib in Japanese patients with an advanced solid tumor; secondary endpoints included safety, pharmacokinetics, and clinical benefit. Results Fifteen patients with an advanced solid tumor were treated. Dose-limiting toxicities of grade 4 neutropenia for ≥7 days and grade 4 thrombocytopenia were both experienced by 2/6 patients in the 350 mg cohort. The MTD of volasertib in Japanese patients was 300 mg.
3.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 E1, Selle F2, Weber B2, Ray-Coquard IL2, Vergote I2, Sufliarsky J2, Del Campo JM2, Lortholary A2, Lesoin A2, Follana P2, Freyer G2, Pardo B2, Vidal L2, Tholander B2, Gladieff L2, Sassi M2, Garin-Chesa P2, Nazabadioko S2, Marzin K2, Pilz K2 J Clin Oncol. 2016 Mar 1;34(7):706-13. doi: 10.1200/JCO.2015.62.1474. Epub 2016 Jan 11.
PURPOSE: Volasertib is a potent and selective cell-cycle kinase inhibitor that induces mitotic arrest and apoptosis by targeting Polo-like kinase. This phase II trial evaluated volasertib or single-agent chemotherapy in patients with platinum-resistant or -refractory ovarian cancer who experienced failure after treatment with two or three therapy lines.
4.Polo-like Kinase Inhibitor Volasertib Exhibits Antitumor Activity and Synergy with Vincristine in Pediatric Malignancies.
Abbou S1, Lanvers-Kaminsky C2, Daudigeos-Dubus E1, LE Dret L1, Laplace-Builhe C3, Molenaar J4, Vassal G1, Geoerger B5; within the ITCC Biology and Preclinical Evaluation Committee. Anticancer Res. 2016 Feb;36(2):599-609.
BACKGROUND: Polo-like kinase 1 (PLK1) controls the main cell-cycle checkpoints, suggesting utility of its inhibition for cancer treatment, including of highly proliferative pediatric cancer. This preclinical study explored the selective PLK1 inhibitor volasertib (BI 6727) alone and combined with chemotherapy in pediatric malignancies.
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CAS 755038-65-4 Volasertib

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