MMAF (hydrochloride)

MMAF (Monomethylauristatin F) hydrochloride is a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF hydrochloride is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as Vorsetuzumab mafodotin and SGN-CD19A^[1][2][3]. IC50 & Target:IC50: 119 nM (Cytotoxicity, Karpas 299 cell), 105 nM (Cytotoxicity, H3396 cell), 257 nM (Cytotoxicity, 786-O cell), 200 nM (Cytotoxicity, Caki-1, cell)^[4] In Vitro:MMAF inhibits anaplastic large cell lymphoma Karpas 299, breast carcinoma H3396, renal cell carcinoma 786-O and Caki-1 cells with IC₅₀s of 119, 105, 257 and 200 nM in vitro cytotoxicity assay^[4]. In Vivo:The maximum tolerated dose in mice of MMAF (>16 mg/kg) is much higher than MMAE (1 mg/kg). cAC10-L1-MMAF₄ has an MTD of 50 mg/kg in mice and 15 mg/kg in rats. The corresponding cAC10-L4-MMAF₄ ADC was much less toxic, having MTDs in mice and rats of >150 mg/ kg and 90 mg/kg in rats, respectively^[4].