Archive for the ‘biotech’ Category
Posted by kinasepro on August 10, 2007
WO/2007/089192 is a use app, and WO/2007/089191 is salt forms application of the pictured GSK3 inhibitor originally from WO/2003/08285. The YM-231146 / YM-359445 series bears similarity, albeit for Vegf.
Posted by kinasepro on August 9, 2007
The news today is that LS-104 is in Ph1 and now owned by Aegera from Lymphosign who in turn licsensed it from HSC. Their portfolio of patent applications suggests the compound is likely a tyrphostin derivative.
LS104 is a novel small molecule tyrosine kinase inhibitor of therapeutically significant kinases including Jak2 and Bcr-Abl…In contrast to marketed kinase inhibitor drugs, LS104 inhibits its targets in a non-ATP-competitive manner
I don’ t know about you but I needed a history lesson to get a handle on these…
Posted by kinasepro on July 13, 2007
wt Abl 1.5 nM
T315I 18 nM
So you like pictures?
Posted by kinasepro on June 21, 2007
Kinex filed an IND today for this ‘ere compound:
KX-01, KX2-391, ALB-30350, wait, ALB-30350? yah…
Note that KX2-391 has weak activity against isolated kinases because the peptide binding site is not well formed outside of cells (a close analog, KX2-394 is a little more potent against isolated Src [KP note: 394 is the piperazine]), but have very potent activity inside whole cells. Without wishing to be bound by theory, it is thought that the difference in activity is attributed to the fact that the peptide binding site is now fully formed in cells due to the allosteric effects of the binding protein partners in the multi-protein signaling complexes, relative to isolated kinase assays.
Posted by kinasepro on June 1, 2007
Posted by kinasepro on May 23, 2007
Posted by kinasepro on May 17, 2007
Supergen just gave an update in Italy yesterday: webcast here. Skip to ~7 minutes for the kinase portion. The highlight for me is on MP-470 where he says that its uM on met (and ret).
but at AACR last year they suggested that:
In their defence I’ll postulate that they meant 4,000 nM concentrations last year. Ultimately does it matter? Only in so far as how much you can trust what they say… heh
Posted by kinasepro on May 2, 2007
Also goes by: API-2, NSC-154020, TCN-P, and triciribine phosphate. and yeh, somebody got the structure wrong in Cancer Res. 04, 4394
(KSR v. Teleflex? suck it.)
Posted by kinasepro on April 17, 2007
1E7U shows the natural product covalently bound to Pi3k