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Enzymes for Research, Diagnostic and Industrial Use

BI6727 (Volasertib)

Cat No.
CEI-0306
Description
BI 6727 potently inhibited Plk1 as well as the two closely related kinases Plk2 and Plk3 (IC 50 values 0.87, 5, and 56 nmol/L, respectively).
CAS No.
755038-65-4
Molecular Weight
618.81
Purity
>99%
Storage
2 years at -20centigrade Powder
Targets
PLK1, PLK2, PLK3
Molecular 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
Solubility
DMSO 50 mg/mL Water
In vitro
BI 6727 potently inhibited Plk1 as well as the two closely related kinases Plk2 and Plk3 (IC 50 values 0.87, 5, and 56 nmol/L, respectively). BI 6727 inhibited proliferation of multiple cell lines derived from various cancer tissues, including carcinomas of the colon (HCT 116, EC 50 = 23 nmol/L) and lung (NCI-H460, EC 50 =21 nmol/L), melanoma (BRO, EC 50 = 11 nmol/L), and hematopoietic cancers (GRANTA-519, EC 50 = 15 nmol/L; HL-60, EC 50 =32 nmol/L; THP-1, EC 50 = 36 nmol/L and Raji, EC 50 =37 nmol/L) with EC 50 values of 11 to 37 nmol/L.
In vivo
In human carcinoma xenografts in nude mice, consecutive cycles of treatment with BI 6727 given oral or i.v. for up to 6 weeks were efficacious in multiple xenograft models. After oral administration comparing three different administration schedules (once a week, twice a week, or daily). At a total weekly dose of 50 mg/kg, all treatment schedules showed comparable efficacy and were well tolerated. In the same model, i.v. Administration of a daily dose of 15, 20, or 25 mg/kg on 2 consecutive days per week led to significant tumor growth delay and even tumor regression.
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