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Key Documents

SML3641

Sigma-Aldrich

Volasertib

≥95% (HPLC)

Synonym(s):

BI 6727, BI-6727, BI6727, N-[trans-4-[4-(Cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxybenzamide

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About This Item

Empirical Formula (Hill Notation):
C34H50N8O3
CAS Number:
Molecular Weight:
618.81
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

Assay

≥95% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear (Warmed)

storage temp.

-10 to -25°C

Biochem/physiol Actions

Volasertib (BI 6727) is an orally active, ATP-competitive, potent and selective polo-like kinase (PLK) inhibitor (PLK1/2/3 IC50 = 0.87/5/56 nM by kinase assay with 7.5 μM ATP) with no significant inhibitory potency (at 10 μM) toward a panel of >50 other kinases. Volasertib exhibits antiproliferation efficacy in cancer cultures (IC50 from 11 to 37 nM) and in mice in vivo via i.v. (20-30 mg/kg/wk or 10-25 mg/kg 2x a wk; HCT-116 & CXB1 xenografts) or p.o. (7-10 mg/kg/d, 15-25 mg/kg 2x a wk, 50-70 mg/kg/wk; NCI-H460, HCT-116 & CXB1 xenografts).

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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