SML3641

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
• Empirical Formula (Hill Notation): C₃₄H₅₀N₈O₃
• CAS Number: 755038-65-4
• Molecular Weight: 618.81
• MDL number: MFCD20926414
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear (Warmed)
• storage temp.: -10 to -25°C

Description

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).

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable