Kinase Chemistry – Just a year and a half behind the times.


Posted by kinasepro on March 27, 2009

Schering-Plough’s CDK1,2,5,9 inhibitor in Ph2 for lung cancer:


WO/2009/038701 has quite a bit to say about the clinical protocol including human PK and a very clean dose response measuring BrdU incorporation.

5 Responses to “SCH-727965”

  1. lowly_modeler said

    Is that be an N-oxide?

  2. abc said

    Does N-oxide have membrane permeability?

  3. kinasepro said

    Yep, its the N-Oxide, and Yep it’s permeable. They go to great lengths to describe the existence of the molecule’s kinase potency (cdk1 4nM, CDK2 1 nM, CDK5, 1 nM, CDK9 4 nM) & cell potency (“…inhibitiion of CDK2/CDK1 in tumor cells leading to cell cycle arrest and apoptosis in more then 100 tumor cell lines including the standard NCI panel…”), and even PK/PD. Surprisingly they don’t confirm or deny if the pyridyl is detected as a metabolite.

  4. Arno said

    The N-oxide could also be a way to increase aqueous solubility, other than the basic aliphatic amines seen so frequently in kinase inhibitors.

  5. Blasphemous pentavalent nitrogen representation…

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