Roscotivine: The Saga

mmm KinaseBlogging:

Part 1, 2, 3, & 4

SCH-727965

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.

Postcards from Vienna…

Hey look what I got:

Yah, its the disclosure of the discovery of PHA-848125.  Not only that, its a pretty good poster. This also means I was wrong again!

Astex: An Oral Candidate for CDK2

Astex’s fragment based discovery effort yielded an oral candidate back in ’05, and now with WO/2007/129066 & WO/2007/129062 the world can have a look. It’s probably AT-9311 even though I could’a swore I heard’m say that their Novartis’ partnered material was of a different series then AT-7519. Perhaps its 7519 I have wrong…

pM CDK2

0.22 uM GSK3b

Mouse: 40-50%F (DMSO/Water/PEG 1/2/7)

Nerviano ‘n CDK

>> Update >> its really PHA-848125

WO/2007/90794 is a CDK inhibitor in combination with yada yada… from Nerviano.  The single compound claimed is pictured and potentially the phase one compound: PHA-793887.

Discovery: Pharmacia IT WO/2004/104007

/. does CDK5

For my read, the story is less that MIT CURES PHEAR! and more that, heh – slashdot picked up a kinase related press release – then proceeded to mangle it. 😦 Nobody tell Derek.

In our study, we employ mice to show that extinction of learned fear depends on counteracting components of a molecular pathway involving the protein kinase Cdk5

MIT Press release; Nature Neuroscience; Falculty page