BI6727 Inhibitor CAS No. 755038-65-4

Cat. No.	Name	Size	Price
KI0075	BI6727	5 mg	$192
	BI6727	10 mg	$336
	BI6727	50 mg	$1072

Chemical Characteristic

Product Name	BI6727
Synonyms	Volasertib
CAS No.	755038-65-4
Molecular Weight	618.81
Formula	C₃₄H₅₀N₈O₃
Chemical Name	N-((1r,4r)-4-(4-(cyclopropylmethyl)piperazin-1-yl)cyclohexyl)-4-((R)-7-ethyl-8-isopropyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-ylamino)-3-methoxybenzamide
Smiles	C(=O)(c1cc(c(cc1)Nc1nc2c(cn1)N(C(=O)[C@H](N2C(C)C)CC)C)OC)NC1CC[C@@H](CC1)N1CCN(CC1)CC1CC1
Chemical Structure

Biological activities

BI6727 is a potent and selective cell-cycle kinase inhibitor that induces mitotic arrest and apoptosis by targeting Polo-like kinase (Plk).^[1] The IC50 of BI6727 is 0.87, 5, and 56 nM against Polo-like kinase 1 (Plk 1), Plk2 and Plk3, respectively. BI6727 inhibits proliferation of multiple cell lines derived from various cancer tissues, including carcinomas of the colon, lung, and melanoma cancer cells. The EC50 of BI6727 is 23, 21 and 11 nM, against HCT116, NCI-H460 and BRO cell, respectively. In addition, BI6727 inhibits hematopoietic cancers including GRANTA-519, HL-60, THP-1 and Raji cells with EC50 of 15, 32, 36 and 37 nM, respectively. Treatment of NCI-H460 cells with increasing concentrations of BI6727 for 24 hours results in accumulation of cells with 4N DNA content.^[1] BI6727 is a second-in-class kinase inhibitor targeting serine/threonine-protein kinase PLK1.^[2] BI6727 induces cellular effects, such as G_{2?? cell-cycle block, phospho-histone H3??ositive staining, and monopolar mitotic spindles.^[3] BI6727 reveals marked antitumor activity in multiple cancer models, including a model of taxane-resistant colorectal cancer. With oral and i.v. routes of administration, the total weekly dose of BI6727 is most relevant for efficacy. BI6727 has a pharmacokinetic profile favoring sustained exposure of tumor tissues with a high volume of distribution and a long terminal half-life in mice and rats. The Vss (volume of distribution in steady state) and t_{1/2 of BI6727 are 7.6 L/kg and 46 hours in mice while that of BI6727 are 22 L/kg and 54 hours.^[1]}}

Protocols

BI6727 is resuspended in 0.5% Natrosol 250 hydroxyethyl-cellulose .^[1]

References

[1] Rudolph D, et al. BI 6727, a Polo-like kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity. Clin Cancer Res. 2009, 15(9): 3094-3102. [2] Spankuech, B. et al. Volasertib. Serine/threonine-protein kinase PLK1 inhibitor, Oncolytic. Drugs Fut. 2012, 37(7): 489. [3] Medema RH, et al. Polo-like kinase 1 inhibitors and their potential role in anticancer therapy, with a focus on NSCLC. Clin Cancer Res. 2011, 17(20): 6459-6466.

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