Cabazitaxel-D6 is a deuterium labeled cabazitaxel. Cabazitaxel (T2543) is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity. Cabazitaxel (T2543)binds to and stabilizes tubulin,resulting in the inhibition of microtubule depolymerization and cell division,cell cycle arrest in the G2/M phase,and the inhibition of tumor cell proliferation. Unlike other taxane compounds,this agent is a poor substrate for the membrane-associated,multidrug resistance (MDR),P-glycoprotein (P-gp)efflux pump and may be useful for treating multidrug-resistant tumors. In addition,cabazitaxel penetrates the blood-brain barrier (BBB).
THR-18 is an 18-mer peptide derived from the sequence of human plasminogen activator inhibitor 1 (PAI-1), having the ability to bind to a site of tissue plasminogen activator (tPA) distal to its catalytic site and uncouple the beneficial clot-dissolving properties of tPA from its deleterious non-fibrinolytic effects.