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 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 Halistatin 1 has highly potent cytotoxic activity
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.
of 4×10-4 μg/mL) and against 60 human cancer cell
lines from the NCI’s anti-tumor screening panel (average overall panel
GI50 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
GI50 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 (GI50, 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:
Benefits and Advantages
confirmed very potent candidates for anti-cancer drugs.
anti-mitotic activities.