KinasePro

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

Archive for November 23rd, 2007

Astex: An Oral Candidate for CDK2

Posted by kinasepro on November 23, 2007

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…

O=C(C2=NNC=C2NC(C3=C(Cl)C=CC=C3Cl)=O)NC1CCN(S(=O)(C)=O)CC1.O=C(C5=NNC=C5NC(C6=C(Cl)C=CC=C6Cl)=O)NC4CCNCC4.N7=CC=CN7

pM CDK2
0.22 uM GSK3b
Mouse: 40-50%F (DMSO/Water/PEG 1/2/7)

Posted in Astex, CDK, CDK2 | 12 Comments »