KinasePro

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

R763

Posted by kinasepro on February 13, 2007

Rigel’s Aurora inhibitor R-763 going Ph1 for ‘Hematological Malignancies’. It’s in Ph1 for solid tumors already. hmm… I thought they had to call it ‘EMD Serono’ in USA.  Merck DE # is: AS703569

So it’s looking like: WO/2006/055561 and before that: WO/2005/118544

FC1=CN=C(NC2=CC(C)=C(N3CCN(C)CC3)C=C2)N=C1N[C@@H]4[C@H](C5)C=C[C@H]5[C@@H]4[C@@](N)=O

Neeto – looks like they resolve the enantiomers via:

Even neeter-0 they show a couple xenos

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2 Responses to “R763”

  1. Are Colo205 cells tough little suckers? The reduction in tumour volume doesn’t appear to be all that special, although to give them credit they didn’t try and massage the data by going in at 100 mg/kg, which I have seen done on more occasions than I care to remember!

  2. kinasepro said

    Not my forte, but I believe colo205 is considered a fast growing cell line, so one reason people look at it because its a quick way to see if your compounds are doing anything. Afaik it’s not considered a very high hurdle. My guess is that they put that experiment in the patent application for promotional reasons to show statistical significance with 7 days dosing.

    Sugen showed colo205 regression with SU11248 (Sutent) in this paper, but not only is that at 80 mg / kg and the time point much longer, but they also waited to start dosing until the tumors were much larger. Its around 30 mg/kg qd that it flatlines the cell line, but an interesting counterpoint is that Nexavar sux-trux against it.

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