WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 204670
Description: BI 811283 is a small molecule inhibitor of the serine/threonine protein kinase Aurora kinase with potential antineoplastic activity. Aurora kinase inhibitor BI 811283 binds to and inhibits Aurora kinases, resulting in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregation, and inhibition of cell proliferation.
MedKoo Cat#: 204670
Synonym: BI811283; BI-811283; BI 811283.
IUPAC/Chemical Name: NONE
BI 811283 is being developed by Boehringer Ingelheim for use as an anti-cancer agent. BI 811283 is currently in the early stages of clinical development and is undergoing first in human trials in patients with solid tumors and Acute Myeloid Leukaemia.
BI 811283 is a small molecule drug that selectively binds to the ATP binding pocket of the Aurora B Kinase protein, inhibiting its function in cell division. The Aurora B kinase protein (also known as STK12) is one of a family of proteins that plays an essential role in the alignment, movement and separation of chromosomes during cell division. Aurora B kinase is produced in all dividing cells in normal tissue however; the levels of Aurora B kinase are abnormally raised in many types of cancer. Abnormally elevated levels of Aurora B kinase, cause unequal chromosomal separation during cell division, resulting in the formation of cells with abnormal numbers of chromosomes, which are both a cause and driver of cancer. Inhibition of Aurora B kinase by BI 811283 in cancer cells leads to the formation of cells with severely abnormal numbers of chromosomes (polyploid). Counterintuitively, inhibition of Aurora B kinase by BI 811283 actually causes the polyploid cells formed to continue dividing however, because these cells have severe chromosomal abnormalities, they eventually stop dividing or undergo cell death. (source: http://en.wikipedia.org/wiki/BI811283).