产品描述
D8-MMAF is a microtubule destroyer, deuterated form of MMAF.
体外活性
MMAF showed cytotoxicity in vitro against a group of cell lines. Karpas 299, H3396, 786-O and Caki-1 have IC50 values of 119, 105, 257 and 200 nM, respectively. Targeted MMAF is more effective than free drug, and the cAC10 conjugate of MMAF shows significant activity. On a molar basis, the average potency of cAC10-L1-MMAF4 is more than 2200 times higher than free MMAF, and it is active in all tested CD30 positive cell lines.
体内活性
The maximum tolerated dose of MMAF (>16 mg / kg) mice is much higher than that of MMAE (1 mg / kg). The MTD of cAC10-L1-MMAF4 is 50 mg / kg in mice and 15 mg / kg in rats. The corresponding cAC10-L4-MMAF4 ADC is much less toxic, with MTD greater than 150 mg / kg and 90 mg / kg in mice and rats, respectively.
Cas No.
T10949
分子式
C39H57D8N5O8
分子量
740.01
别名
Monomethylauristatin F D8;D8-MMAF
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years