4sc207

4SC-207 is a novel microtubule inhibitor , which shows strong anti-proliferative activity in a large panel of tumor cell lines with an average GI50 of 11 nM. In particular, 4SC-207 is active in multi-drug resistant cell lines, such as HCT-15 and ACHN, suggesting that it is a poor substrate for drug efflux pumps. 4SC-207 inhibits microtubule growth in vitro and in vivo and promotes, in a dose dependent manner, a mitotic delay arrest, followed by apoptosis or aberrant divisions due to chromosome alignment defects and formation of multi-polar spindles. Furthermore, preliminary data from preclinical studies suggest low propensity towards bone marrow toxicities at concentrations that inhibit tumor growth in paclitaxel-resistant xenograft models. 4SC-207 may be a potential anti-cancer agent.

ODM-207 (BET-IN-4) is a potent inhibitor of BRD4.

GNE-207 is a selective and orally bioavailable inhibitor of the bromodomain of CBP (IC50: 1 nM). It has a selective index of >2500-fold against BRD4 (1). GNE-207 displays excellent CBP potency (EC50: 18 nM for MYC expression in MV-4-11 cells).

4'-hydroxy Atomoxetine glucuronide is a metabolite of the norepinephrine transporter (NET) inhibitor atomoxetine .1It is formed from atomoxetine by glucuronidation of the intermediate metabolite 4-hydroxy atomoxetine.2 1.Todor, I., Popa, A., Neag, M., et al.Evaluation of a potential metabolism-mediated drug-drug interaction between atomoxetine and bupropion in healthy volunteersJ. Pharm. Pharm. Sci.19(2)198-207(2016) 2.Sauer, J.-M., Ring, B.J., and Witcher, J.W.Clinical pharmacokinetics of atomoxetineClin. Pharmacokinet.44(6)571-590(2005)