BI-2536, PLK1 and BRD4 Dual Inhibitor


Catalog No. size PriceQuantity
M60171-5S 5 mg solid $119
M60171-10S 10mg solid $312

Description

Product Information
Molecular Weight: 521.65
Formula: C28H39N7O3
Purity: ≥98%
CAS#: 755038-02-9
Solubility: DMSO up to 40 mM
Chemical Name: (R)-4-((8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl)amino)-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

BI-2536 is a potent inhibitor of PLK1 (Polo-like kinase 1, IC50 ~0.83 nM) and BRD4 (IC50 ~37 nM).  It also inhibits PLK2 and PLK3 with IC50 of 3.5 nM and 9.0 nM, respectively. BI-2536 treatment ranging from 10 nM to 100 nM leads to the blocking of the recruitment of γ-tubulin and phosphorylation of Apc6 at mitotic centrosomes, inhibition of cohesin release from chromosome arms, induction of monopolar spindles, and other Plk1 dependent processes. BI-2536 inhibits the growth of a panel of 32 human cancer cell lines with EC50 of 2-25 nM. It also displaces BRD4 from chromatin and suppresses c-Myc expression. The combination of inhibitory activities on independent kinase and bromodomain oncogenic pathways exemplifies a new strategy for rational single-agent polypharmacological targeting. 

 

How to Use:

In vitro:  BI-2536 was used at 0.1-1 µM in vitro.

In vivo:  BI-2536 was dosed to mice by IV injection at 50 mg/kg once or twice a week in xenograft models. (Formulated in hydrochloric acid (0.1 N), and diluted with 0.9% NaCl)

 

Reference: 

  1. Steegmaier M, et al. BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo. (2007) Curr Biol. 17(4):316-22.
  2. Nappi TC, et al. Identification of Polo-like kinase 1 as a potential therapeutic target in anaplastic thyroid carcinoma.  (2009) Cancer Res. 69(5):1916-23.
  3. Ciceri P, et al. Dual kinase-bromodomain inhibitors for rationally designed polypharmacology. (2014) Nat Chem Biol. In press. 

 

Products are for research use only. Not for human use.

 

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