A dihydropteridinone that inhibits Plk1

BI-6727 – 5 mg

Brand:
Cayman
CAS:
755038-65-4
Storage:
-20
UN-No:
Non-Hazardous - /

Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.{29228} BI-6727 is a dihydropteridinone that inhibits Plk1, Plk2, and Plk3 (IC50s = 0.87, 5, and 56 nM, respectively), inducing mitotic arrest and apoptosis.{29375} It inhibits proliferation of multiple cancer cell lines with EC50 values ranging from 11-37 nM and prevents the growth of various human carcinoma xenografts in mice.{29375} BI-6727 was found to reverse ABC-efflux transporter-mediated multidrug resistance activity through its inhibition of the transport activity of ABCB1 and ABCG2, thus promoting mitotic arrest in resistant cancer cells.{29376}  

 

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Description

A dihydropteridinone that inhibits Plk1, Plk2, and Plk3 (IC50s = 0.87, 5, and 56 nM, respectively), inducing mitotic arrest and apoptosis; inhibits proliferation of multiple cancer cell lines (EC50s = 11-37 nM) and prevents the growth of various human carcinoma xenografts in mice

Formal name: 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-methoxy-benzamide

Synonyms:  Volasertib

Molecular weight: 618.8

CAS: 755038-65-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Plks||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|PLK Signaling

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