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

Archive for the ‘EGF’ Category


Posted by kinasepro on April 13, 2009

Aveo’s Ph1 irreversible  Erbb inhibitor:


via Mitsubishi

Posted in EGF | 2 Comments »


Posted by kinasepro on March 16, 2009

aka: NVP-AEE788 is Novartis’ VEGF / EGF ‘Nib (&src, &flt, etc.) in Ph1 for the last 6 years… and unceremoniously off the pipeline.


Cancer Res

Posted in EGF, Novartis, VEGF | Leave a Comment »


Posted by kinasepro on October 22, 2008

Exel’s got Pi3K-a in combination: Reminds one of the XL-147 combo study.


So thats XL-647 ?  I hadn’t heard.

Posted in EGF, Exelixis, pi3k | Leave a Comment »

PDB Update

Posted by kinasepro on December 5, 2007

Berkeley’s got a Nature 2007, 450, 741 on a peptide that inhibits EGF 

and the PDB’s released yesterday: 2RFD 3.6 Å, 2RF9 3.5 Å, 2RFE 2.9 Å

To understand what they’re talking about I had to read the earlier piece in Cell.   You could probably just skip it because the Monkey Wrench breaks it down for you.

Posted in EGF | 1 Comment »

Bayer ‘n Egf

Posted by kinasepro on October 2, 2007

Set of covalent ErbB inhibitors from Bayer:



Posted in Bayer, EGF | 3 Comments »


Posted by kinasepro on September 7, 2007

BI’s irreversible ErbB inhibitor to join the Ph3 club.


>> update they’ve named it Tovok

Posted in BI, EGF, Phase III | 4 Comments »

More Her

Posted by kinasepro on August 21, 2007

‘nother ErbB 1,2,4 crystal forms app from BMS in US20070191375:


Posted in BMS, EGF | 2 Comments »

ARRY-380: an Array ErbB2 IND

Posted by kinasepro on August 4, 2007

IND: in the books, Market: not impressed. If you’ve been paying attention you already noticed Array’s got ‘n’ ErbB series published 5/24: WO/2007/059257



ARRY-380, a selective, orally-active ErbB-2 inhibitor, has shown efficacy and is well-tolerated in preclinical models of human cancer.

Posted in Array, EGF | 1 Comment »

Oximes from J&J

Posted by kinasepro on July 22, 2007

So J&J has a BMCL describing the amino-pyrimidine-oxime moiety as quinazoline isostere, and a there’s a handful of other applications describing the motif.   Here’s a Lapatinib-esque example where they describe the EGF activity: WO/2007/081630


< 2g/d plz

Posted in EGF, J&J | 6 Comments »


Posted by kinasepro on June 19, 2007

aka vandetanib, ZD-6474 is Astra’s Vegf / EGF doublet inhbitor.


wiki, clinic, WO/2001/032651

Posted in Astra, EGF, Phase III, VEGF | 1 Comment »