Volasertib, Potent and selective inhibitor of Polo-like Kinase 1 (TBI4818)

Description

Product Details

Formal Name: N-[4-[4-(Cyclopropylmethyl)piperazin-1-yl]cyclohexyl]-4-[[(7R)-7-ethyl-5-methyl-6-oxo-8-propan-2-yl-7H-pteridin-2-yl]amino]-3-methoxybenzamide

Alternate Names: BI 6727

Molecular Formula: C₃₄H₅₀N₈O₃

Formula Weight: 618.82

CAS Number: 755038-65-4

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

 

Applications

Potent and selective inhibitor of Polo-like Kinase 1

 

Functions

Volasertib is an extremely potent and selective inhibitor (IC50’s: Plk1= 0.87 nM, Plk2 = 5 nM, Plk3 = 56 nM) of Polo-like kinase , a critical controller of multiple essential steps of mitosis. It has shown efficacy in multiple solid xenograft tumors models and in clinical studies in patients with acute myeloid leukemia. Volasertib has also been shown to potently inhibit BRD4 (Kd = 79 nM, IC50’s bromodomains 1 and 2 of BRD4 = 300 and 770 nM respectively).

 

Application Procedures

First dissolved in DMSO (up to at least 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20° for up to 1 month.

Additional information

SIZE (mg)	25 MG, 5 MG

Datasheet:

TBI4818_Volasertib

MSDS:

TBI4818_Volasertib_MSDS_2024