Volasertib(BI6727)

Cas No.:	755038-65-4
Chemical Name:	Volasertib
Synonyms:	BI 6727; BI-6727; BI6727
SMILES:	CC[C@@H]1C(=O)N(C2=CN=C(N=C2N1C(C)C)NC3=C(C=C(C=C3)C(=O)NC4CCC(CC4)N5CCN(CC5)CC6CC6)OC)C
Formula:	C34H50N8O3
M.Wt:	618.81
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	Volasertib is a highly potent Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM, as well as the two closely related kinases PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively.
In Vivo:	Volasertib (15 mg/kg, i.p.) potentiates the activity of cisplatin to inhibit xenograft tumor growth of cervical cancer cells in nude mice[1]. Volasertib (70 mg/kg, p.o. once a week or 10 mg/kg, p.o. daily) significantly delays tumor growth in a non-small cell lung carcinoma xenograft model. In addition, Volasertib (15 mg/kg, i.v.) markedly suppresses tumor growth and is well tolerated[3].
In Vitro:	Volasertib is potent against HeLa and Caski cells with IC50 values of 0.02 μM and 2.02 μM, respectively. Volasertib (0.03 μM) induces cell cycle arrest at G2/M Phase in cervical cancer cells. Volasertib (0.003-0.03 μM) induces apoptosis in HeLa cells, and Volasertib (0.3-3 μM) results in Caski cell apoptosis. Volasertib (1, 3 μM or 0.01,0.03 μM) augments the fluorescent intensity of DHE in Caski and HeLa cells in a dose-dependent manner[1]. Volasertib shows inhibitory activities against the proliferation of all 40 cell lines tested, with a mean half-maximal growth inhibitory concentration of 313 nM (range: 4-5000 nM)[2]. Volasertib inhibits proliferation of multiple cell lines derived from various cancer tissues, including carcinomas of the colon (HCT 116, EC50=23 nM) and lung (NCI-H460, EC50=21 nM), melanoma (BRO, EC50=11 nM), and hematopoietic cancers (GRANTA-519, EC50=15 nM; HL-60, EC50=32 nM; THP-1, EC50=36 nM and Raji, EC50=37 nM) with EC50 values of 11 to 37 nM. Volasertib (100 nM) causes G2-M arrest and induces apoptosis in NCI-H460 cells[3].