KinasePro

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

Pazopanib

Posted by kinasepro on May 13, 2007

aka GW-786034 is GSK’s ‘pan Vegfr’ / TIE2 inhibitor:

O=S(C1=CC(NC2=NC=CC(N(C)C3=CC4=NN(C(C)=C4C=C3)C)=N2)=CC=C1C)(N)=O

salt: hydrochloride
some chemistry here.
clinic: ph ii, WO/2002/059110

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2 Responses to “Pazopanib”

  1. KinaseNerd said

    It’s a pan VEGF inhibitor, agreed. In addition it hits the PDGFRs and cKit. Check out Curr. Oncol. Rep. 2007, 9, 115. Haven’t heard about TIE as a pazopanib target. There seems to be some buzz about TIE in the IP world. But is it of any relevance in the clinics?

  2. kinasepro said

    Hmm, its in my notes and I had to double check why. Afaik they haven’t published an ic50 on Tie2. {Curr Onc subscription is unfair to me ;/} Claims 75 and 76 of the initial application suggests that they were indeed looking at it within the series, but as for the compound… dunno.

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