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simotaxel

A semi-synthetic, orally bioavailable, third-generation taxane derivative and microtubule-stabilizing agent, with potential antineoplastic activity. Upon administration, simotaxel binds to tubulin, promotes microtubule assembly and stabilization, and prevents microtubule depolymerization. This results in G2/M arrest, apoptosis and the inhibition of cell proliferation in susceptible tumor cells. This agent is a poor substrate for P-glycoprotein-related drug resistance mechanisms; therefore, it may be useful for treating multi-drug resistant tumors. MST-997 is more potent than paclitaxel and docetaxel and overcomes paclitaxel and docetaxel resistance in certain tumor cell types.
Synonym:taxane-997
Code name:MST-997
TL-909
Chemical structure:5Beta,20-epoxy-1,2alpa,4,7beta,10beta,13alpha-hexahydroxytax-11-en-9-one-4-acetate 2-benzoate Ester with (2R,3S)-N-Isopropoxycarbonyl-3-(2-thienyl) isoserine
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