7239453

Tocris Bioscience™ Adavosertib

Potent and selective Wee1 inhibitor

Manufacturer: Fischer Scientific

CAS Number: 955365-80-7

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Chemical Name or Material

1,2-Dihydro-1-[6-(1-hydroxy-1-methylethyl)-2-pyridinyl]-6-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-2-(2-propen-1-yl)-3 H-pyrazolo[3,4-d]pyrimidin-3-one

Target

Checkpoint Control Kinase Inhibitors

Purity

98%

CAS

955365-80-7

Molecular Formula

C27H32N8O2

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Description

  • Adavosertib is a potent and selective Wee1 inhibitor (IC50 = 5.2 nM)
  • In a panel of 223 serine/threonine or tyrosine kinases, Adavosertib is highly selective for Wee 1 over all except 8 kinases
  • In particular Adavosertib shows >100-fold selectivity over human Myt1
  • Adavosertib blocks CDC2Y15 phosphorylation and Gemcitabine (Cat
  • No
  • 3259)-induced DNA damage checkpoint, leading to premature mitotic entry and apoptosis in p53-deficient tumor cell lines
  • Adavosertib also potentiates the cytotoxic effects of Pemetrexed (Cat
  • No
  • 6185), Doxorubicin (Cat
  • No
  • 2252), Camptothecin (Cat
  • No
  • 1100) and Mitomycin C (Cat
  • No
  • 3258) in vitro
  • Adavosertib synergizes with gemcitabine to achieve tumor regressions, selectively in p53-deficient pancreatic cancer xenografts.

SAFETY INFORMATION

  • Recommended Storage : Store at -20°C