Case ID: Halistatins

Published: 2010-03-22 12:00:02

Last Updated: 1661888621


Inventor(s)

George (Bob) Pettit

Technology categories

Life Science (All LS Techs)

Technology keywords

Cancer
Natural Product


Licensing Contacts

Tom Goodman
President
[email protected]
480-884-1648

Halistatins 1, 2 & 3




Contact


Jack Geltosky, PhD


Senior Vice President of Business Development, Life Sciences


Arizona Technology Enterprises, LLC (AzTE)


P: 480.884.1989


F: 480.884.1984


[email protected]


Inventors


George Pettit, PhD


Regents Professor


Department of Chemistry and Biochemistry


Arizona State University


Rui Tan


Feng Gao


Yoshitatsu Ichtihara


Halistatins 1, 2 and 3


AzTE Cases # 626, 627, 701


Intellectual Property Status:


U.S. Patent 5,426,194


U.S. Patent 5,352,804


U.S. Patent 5,519,050


Invention Description


Halistatins are highly potent polyether macrolides with
anti-mitotic actions that were originally isolated from certain marine sponges.
Similar polyether macrolides, such as, Bryostatin 1 (Ph2), Halichondrin B (PC)
and its analog, E7389 (Ph 2), are being tested both preclinically and clinically
as anti-cancer agents.


Halistatin 1 has highly potent cytotoxic activity
in vitro against P388 cells (ED50
of 4×10-4 μg/mL) and against 60 human cancer cell
lines from the NCI’s anti-tumor screening panel (average overall panel
GI
50 of 7×10-10 M).


Halistatin 2 has highly potent cytotoxic activity
in vitro against P388 cells (ED50
of 4×10-4 μg/mL) and against 60 human cancer cell
lines from the NCI’s anti-tumor screening panel (average overall panel
GI
50 of 7×10-10 M).


Halistatin 3 strongly inhibits growth (ED50
of 3.5×10-5 μg/mL) of P388 leukemia cells and a
‘mini’ panel of human cancer cell lines (GI
50, μg/mL): brain (SF-295, 3.5×10-5), lung (NCI-460, 2.5×10-5), colon (KM 2062, 5.1×10-6), ovary (OVCAR-3, 1.3×10-5), renal (A498, 5.6×10-5) and melanoma (SK-MEL-5, 2.5×10-5).


Potential Applications


These novel compounds have applications as:



  1. Anti-cancer therapeutic agents

 


Benefits and Advantages



  1. Diversity – The new compounds are structural analogs of
    confirmed very potent candidates for anti-cancer drugs.


  1. Efficacy – The new compounds also possess promising
    anti-mitotic activities.