MONOMETHYLAURISTATIN F HYDROCHLORIDE

中文名称:

MONOMETHYLAURISTATIN F HYDROCHLORIDE

中文同义词:

细胞分裂抑制剂(MMAF HYDROCHLORIDE)

英文名称:

MMAF (Hydrochloride)

英文同义词:

MMAF (Hydrochloride);Monomethylauristatin F Hydrochloride;MMAF HCl;CS-1270

CAS号:

1415246-68-2

分子式:

C39H66ClN5O8

分子量:

768.42304

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

1415246-68-2.mol

生物活性

MMAF (Monomethylauristatin F) hydrochloride 是一种有效的微管蛋白聚合 (tubulin polymerization) 抑制剂，用作抗肿瘤药物。MMAF hydrochloride 广泛用作抗体偶联药物 (ADCs) 的细胞毒性成分，如 Vorsetuzumab mafodotin 和 SGN-CD19A。

靶点

Auristatin

Auristatin

体外研究

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.

体内研究

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.