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


Posted by kinasepro on May 6, 2009

It’s SGX’s former Ph1 c-Met inhibitor & Derek‘s got a post on it.  Lilly released that the trial was halted due to a reversible acute renal failure in the 80 mg dose group brought on by a compound crystallizing in the kidney.


makes you wonder…

8 Responses to “SGX-523”

  1. anon said

    Any idea about the structure of the backup compound SGX126?

  2. milkshake said

    Fragment-based crystalography technology platform my ass. I think their technology platform never worked as advertised so they proceeded to old-fashioned patent busting… The kidney stones fiasco serves them right, for putting diaryl sulfide in the clinic

  3. kinasepro said

    Who care’s what the solubility of an active metabolite is? It already gets on-board, its like a pro-drug only better!

    oh wait a minute….

    Small biotech doesn’t go Ph1 without a partner unless there’s a reason. The reason’s usually aren’t good. Still what happened to this compound is reasonably unpredictable, though reports are this effect was observed in monkey.

  4. Ed said

    Do you reckon that this metabolite is the diaryl sulfoxide or sulfone?

    My experience of those is that they are generally lovely high melting crystalline solids.

  5. David said

    Completely agree with milkshake!

  6. Arno said

    Is the structure of SGX-523 correct as shown? In light of the structure of the cMet inhibitor from JnJ (ex.61 from WO2007/075567), I would have guessed that the quinoline is substituted at C6 rather than C5.

  7. kinasepro said

    Thanks Arno: I fat fingered it… its now fixed

  8. taylor said

    Apparently it has been terminated…

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