(R)-BI-2536

CHF 96.00
In stock
SYN-1019-M0011 mgCHF 96.00
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SYN-1019-M100100 mgCHF 1'203.00
 
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Product Details
Synonyms (R)-BI2536
Product Type Chemical
Properties
Formula C28H39N7O3
MW 521.7
CAS 755038-02-9
Purity Chemicals ≥95%
Appearance Solid.
Solubility Soluble in DMSO, Ethanol
Declaration Manufactured by SynKinase.
Other Product Data Target: Plk1 | Kinase Group: Other | Substrate: Serine-Threonine

Click here for Original Manufacturer Product Datasheet
Our product description may differ slightly from the original manufacturers product datasheet.
InChi Key XQVVPGYIWAGRNI-JOCHJYFZSA-N
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
Polo-like kinase 1 (Plk1) is a regulator of the cell cycle that has been implicated in the pathology of many cancers. BI-2536 is a potent and selective small-molecule inhibitor of mammalian Plk1. It has inhibitory activity at subnanomolar concentrations and inhibits tumor growth in multiple tumor lines with IC(50) values below 1µM. BI-2536 also shows an >1,000-fold selectivity for PIK1 versus a large panel of other kinases. BI-2536 also demonstrated low Kd values against sister kinases PLK2 and PLK3. Preclinical studies in human cancer cell lines have shown that BI 2536 disrupts spindle assembly, resulting in mitotic arrest and inducing apoptosis. BI-2536 is currently in clinical trials against several types of solid tumor cancers.
Product References
  1. BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo: M. Steegmaier, et al.; Curr. Biol. 17, 316 (2007)
  2. Pharmacophore modeling and virtual screening for designing potential PLK1 inhibitors: H.Y. Wang, et al.; Bioorg. Med. Chem. Lett. 18, 4972 (2008)
  3. Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors: Q. Zhang, et al.; Bioorg. Med. Chem. Lett. 22, 7615 (2012)
  4. HDAC inhibitors increase NRF2-signaling in tumour cells and blunt the efficacy of co-adminstered cytotoxic agents: M. McMahon, et al.; PLoS One 9, e114055 (2014)
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