Abstract
ET-743 is a novel quinoline alkaloid isolated from a caribbean tunicate. IVT studies identifies activity (A) in A549 lung, HT29colon, and Melmelanoma (MEL) cell lines with IC50s=034,0.60 and 0.66nM rescepctivily. The NCI IVT panel coofirmed A particularly in MEL, NSCLC, breast (B) and Ovarian (O) lines. This A has been validated in the IVT-HTCFU assay: 100% and 50% IVT responses for B and O exposed to 1.0uM and 0.0luM respectivily. ET-743 binds to DNA and affects the microtubule network, moreover ET-743 bloks cell cycle progression in late S and G2/M. Initial INV studies confirmed A in early and advanced (MX-I) B xenografts (X) with a complete response (CR) rate=100% and 90% the respectivily. Further INV studies in HOC22 (O), MEXF514 (mel) and LX529 (NSCLC) show impressive A with %T/C
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