D8-MMAF (hydrochloride)
| 中文名称 | D8-MMAF (hydrochloride) |
|---|---|
| 中文同义词 | 化合物 D8-MMAF hydrochloride |
| 英文名称 | D8-MMAF (hydrochloride) |
| 英文同义词 | D8-MMAF (hydrochloride) |
| CAS号 | |
| 分子式 | C??H??D?ClN?O? |
| 分子量 | 0 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | Mol File |
| 结构式 |
D8-MMAF (hydrochloride) 性质
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Auristatin
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MMAF shows in vitro cytotoxicity against a panel of cell lines. The IC 50 values for Karpas 299, H3396, 786-O and Caki-1 are 119, 105, 257, and 200 nM, respectively. Targeted MMAF is much more potent than the free drug, and that cAC10 conjugates of MMAF display pronounced activities. On a molar basis, the cAC10-L1-MMAF 4 is an average of over 2200-fold more potent than free MMAF and is active on all the CD30-positive cell lines tested.
The maximum tolerated dose in mice of MMAF (>16 mg/kg) is much higher than MMAE (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.