Motesanib: A little too good.
Posted by kinasepro on November 20, 2008
Looks like this one might be coming off the ph3 list…
![O=C(NC1=CC=C(C(C)(C)CN2)C2=C1)C3=CC=CN=C3N([H])CC4=CC=NC=C4](http://img230.imageshack.us/img230/6476/amgfw8.jpg)
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Journals (beta)- Synthesis and Biological Evaluation of 3,6-Diamino-1H-pyrazolo[3,4-b]pyridine Derivatives as Protein Kinase Inhibitors
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- 9-(Arenethenyl)purines as Dual Src/Abl Kinase Inhibitors Targeting the Inactive Conformation: Design, Synthesis, and Biological Evaluation
- Identification of Inhibitors of Checkpoint Kinase 1 through Template Screening
- Characterizing the Effects of the Juxtamembrane Domain on Vascular Endothelial Growth Factor Receptor-2 Enzymatic Activity, Autophosphorylation, and Inhibition by Axitinib
- A Study of CDK2 Inhibitors Using a Novel 3D-QSAR Method Exploiting Receptor Flexibility
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Ed said
AZ’s Zactima Phase III data were released yesterday also, and seemed less than impressive to me (no numbers provided – but maybe they are embargoed for an upcoming conference?), with no statistical significance for the OS improvement endpoint.
Orgmed said
AMG-706 is diphosphate. Is this the multi-targeted?. 125 mg per day….?
Lower doses may work.
goldilocks said
Any idea what’s going on with AMG-273?
milkshake said
KinasePro: have you noticed Kinasecentral from CrimsonCanary, http://www.kinasecentral.com/ ?
kinasepro said
read own blog much?
meh. I’ve been performing a silent experiment wondering when she’d get around to linking to KP.
weirdo said
I think you’re going to wait a long time. Linking to free sites when one is trying to sell something is seldom a good idea.
And KinaseCentral needs some quality control. A headline describing a Pfizer disclosure on CP-690,550 links to the JMedChem paper on CP-690,550 from an NIH lab. Reading the by-line helps, ya know?
kinasepro said
Umm, but uh – dude it had the work kinase in it?
milkshake said
I know, just headlines devoid of (free) analysis – but still, there are so many BMCL papers and industry announcements that if someone pre-reads them for me, it saves me from wadding through all that low-grade stuff. I found recently some BCML ASAP articles through KinaseCentral that could actually help us with a project.
Curious Wavefunction said
ROCK inhibitor from Bayer Schering. Current cover of ChemMedChem
DisgruntledViewer said
What do any of these comments have to do with the article? Is this an “educated” website, or is everyone here to advertise and complain about unrelated topics? This article was supposed to be about Motesanib and no one even metions it once…
kinasepro said
Educated? nah… We’re more like the peanut gallery.
milkshake said
…and some people have a peanut allergy. Anyway, I hope that the corporate lawyers and other due-diligence imbeciles won’t harass you for KinasePro, and that you will have energy and time to continue writing about kinase compounds in the next year. Happy holiday!
Woodward said
You people really spend your time talking about and promoting small molecule kinase inhibitors? Highly selective, multi-target, blah, blah, blah. These compounds have killed more rats than Terminex. The highest concentrations of an orally administered kinase inhibitors are in the GI (mM) and the liver (uM)…they saturate the cytosol in the GI and other organs long before they ever make it to target tissue. Intestinal paralysis, elevated liver enzymes, organs swelling and shrinking. The whole kinase inhibitor thrust has been a quagmire. Our collections are now full of kinase inhibitors that have been a complete waste of chemistry resources.
kinasepro said
Aww, I dunno… All those folks on Gleevec don’t seem to mind.
nerdase said
gleevec might evade GI tox partially owing to the fact as a prodrug. its active metabolite is 3~5x more potent. it is curious that few people in the field paid much attent to the later. It could a way to go for future kianse inhibitors. btw sorafenib has 5x and 3x higher accumulation in liver and kidney comparing to blood. no wonder it got approved in hcc and rcc.