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Products are for research use only. Not for human use. We do not sell to patients.

Signaling Pathway

Volasertib

HY-12137

(BI 6727; BI-6727; BI6727)

Volasertib
Volasertib Chemical Structure

Volasertib(BI6727) is a highly potent PLK1 inhibitor with an IC50 of 0.87 nM; shows 6- and 65-fold greater selectivity against Plk2 and Plk3.

Price and Availability of Volasertib
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Volasertib Data Sheet

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Purity: 97.74%

Volasertib

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Biological Activity of Volasertib

Volasertib(BI6727) is a highly potent PLK1 inhibitor with an IC50 of 0.87 nM; shows 6- and 65-fold greater selectivity against Plk2 and Plk3.
IC50 Value: 0.87 nM
Target: PLK1
in vitro: Like BI2536, BI6727 is an ATP-competitive kinase inhibitor from the dihydropteridinone class of compounds. In addition to Plk1, BI6727 also potently inhibits two closely related kinases Plk2 and Plk3 with IC50 of 5 nM and 56 nM, respectively. BI6727 at concentrations up to 10 μM displays no inhibitory activity against a panel of >50 other kinases. BI6727 inhibits the proliferation of multiple cell lines derived from various cancer tissues, including HCT116, NCI-H460, BRO, GRANTA-519, HL-60, THP-1, and Raji cells with EC50 of 23 nM, 21 nM, 11 nM, 15 nM, 32 nM, 36 nM, and 37 nM, respectively. BI6727 treatment (100 nM) in NCI-H460 cells induces an accumulation of mitotic cells with monopolar spindles and positive staining for histone H3 phosphoserine 10, confirming that cells are arrested early in the M phase, followed by induction of apoptosis. Low nanomolar concentrations of BI6727 display potent inhibitory activity against neuroblastoma (NB) tumor-initiating cells (NB TIC) with EC50 of 21 nM, whereas only micromolar concentrations of BI6727 are cytotoxic for normal pediatric neural stem cells. BI6727 induces growth arrest of Daoy and ONS-76 medulloblastoma cells similar to BI 2536.
in vivo: Administration of BI6727 significantly inhibits the growth of multiple human carcinoma xenografts including HCT116, NCI-H460, and taxane-resistant CXB1 colon carcinoma, accompanied by an increase in the mitotic index as well as an increase in apoptosis. In in vivo studies, BI6727 shows better toxicity and pharmacokinetic profile compared to BI2536.

Clinical Information of Volasertib

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[1]. Grinshtein N et al. Small molecule kinase inhibitor screen identifies polo-like kinase 1 as a target for neuroblastoma tumor-initiating cells. Cancer Res. 2011 Feb 15;71(4):1385-95.
[2]. Sch?ffski P, Awada A, Dumez H, Gil T, Bartholomeus S, Wolter P, Taton M, Fritsch H, Glomb P, Munzert G.A phase I, dose-escalation study of the novel Polo-like kinase inhibitor volasertib (BI 6727) in patients with advanced solid tumours.Eur J Cancer. 2012 Jan;48(2):179-86. Epub 2011 Nov 24.
[3]. Rudolph D, Steegmaier M, Hoffmann M, Grauert M, Baum A, Quant J, Haslinger C, Garin-Chesa P, Adolf GR.BI 6727, a Polo-like kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity.Clin Cancer Res. 2009 May 1;15(9):3094-102. Epub 2009 Apr 21.
[4]. Sanhaji M, Kreis NN, Zimmer B, Berg T, Louwen F, Yuan J. p53 is not directly relevant to the response of Polo-like kinase 1 inhibitors.Cell Cycle. 2012 Feb 1;11(3):543-53. Epub 2012 Feb 1.
[5]. Sch?ffski P.Polo-like kinase (PLK) inhibitors in preclinical and early clinical development in oncology.Oncologist. 2009 Jun;14(6):559-70. Epub 2009 May 27.

Products are for research use only. Not for human use. We do not sell to patients.

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