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


Posted by kinasepro on May 28, 2007


Lestaurtinib / CEP-701 is currently in trials for a handful of indications and first appeared in WO/1988/07045 (US,4,923,986) via Kyowa Hakko Kogyo. The series was first described as a group of PKC inhibitors, but later came this ’98 press release: (emphasis mine)

CEP-701 is one of a series of specific receptor trk kinase inhibitor derived from the indolocarbazole K252a, which was originally synthesized by Kyowa Hakko Kogyo Co., Ltd., Tokyo, Japan

It has since been described as a Vegfr-2, FLT-3, Trk-A and JAK-2, but looking at the structure I would be shocked if the list ends there.

3 Responses to “Lestaurtinib”

  1. xtallographer said

    It also hits c-Met (amongst others)

  2. milkshake said

    I though the staurosporine analogs were the oldest and most problematic kinase inhibitor class. It surprises me that some companies are still trying to develop these, when there are so many good scaffolds to chose from. I think kinases are relatively easy to target (as opposed to proteases) so one can afford to be picky, when chosing what to work on.

  3. kinasepro said

    Aww c’mon in ’88 that compound was off the heezey

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