一甲基澳瑞他汀 F用作科学研究和化学试剂等领域。
一甲基澳瑞他汀 F是抗微管药。有力的有丝分裂抑制剂。
MMAF是一种合成的抗肿瘤药物。它是一些实验性抗癌抗体-药物偶联物的一部分,如vorsetuzumab mafodotin和SGN-CD19A。在MMAF-抗体偶联物的国际非专利名称中,mafodotin指的是MMAF及其与抗体的连接结构。MMAF实际上是去甲基奥利斯特汀F;也就是说,N-末端氨基只有一个甲基取代基。
MMAF inhibits anaplastic large cell lymphoma Karpas 299, breast carcinoma H3396, renal cell carcinoma 786-O and Caki-1 cells with IC 50 s of 119, 105, 257 and 200 nM in vitro cytotoxicity assay.
The maximum tolerated dose in mice of MMAF (Monomethylauristatin F) (>16 mg/kg) is much higher than MMAF (Monomethylauristatin F) (1 mg/kg). cAC10-L1-MMAF 4 has an MTD of 50 mg/kg in mice and 15 mg/kg in rats. The corresponding cAC10-L4-MMAF 4 ADC was much less toxic, having MTDs in mice and rats of >150 mg/ kg and 90 mg/kg in rats, respectively.