A selective Plk1 inhibitor (IC50s = 3 and 6 nM in an enzymatic assay and H82 lung cancer cells

Ro 3280 – 10 mg

Brand:
Cayman
CAS:
1062243-51-9
Storage:
-20
UN-No:
Non-Hazardous - /

Ro 3280 is a selective inhibitor of polo-like kinase 1 (Plk1), a proto-oncogene, with IC50 values of 3 and 6 nM in an enzymatic assay and H82 lung cancer cells, respectively.{34562} Ro 3280 is over 500-fold selective for PlK1 over a panel of 318 kinases. It inhibits tumor growth in a mouse xenograft model using the HT-29 colorectal cancer cell line, increases autophagy and mTOR phosphorylation in NB4 acute myeloid leukemia cells, and induces apoptosis in human bladder cancer and leukemia cells.{34562,34563,34565,34564}  

 

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Description

A selective Plk1 inhibitor (IC50s = 3 and 6 nM in an enzymatic assay and H82 lung cancer cells, respectively); over 500-fold selective over a panel of 318 kinases; inhibits tumor growth in a mouse xenograft model; increases autophagy and mTOR phosphorylation in NB4 cells; induces apoptosis in cancer cell lines

Formal name: 4-[(9-cyclopentyl-7,7-difluoro-6,7,8,9-tetrahydro-5-methyl-6-oxo-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide

Synonyms: 

Molecular weight: 543.6

CAS: 1062243-51-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Plks||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Autophagy||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|PLK Signaling||Research Area|Cell Biology|Cell Death|Apoptosis||Research Area|Cell Biology|Endomembrane System & Vesicular Trafficking|Autophagy

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