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MMAF Hydrochloride
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
MMAF Hydrochloride图片
CAS NO:1415246-68-2
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
MMAF hydrochloride (Monomethylauristatin F Hydrochloride) 是抑制细胞分裂的抗微管蛋白剂; 抑制H3397细胞生长的IC50值为105 nM。
Cas No.1415246-68-2
别名Monomethylauristatin F hydrochloride
Canonical SMILESCC(C)[C@H](NC)C(N[C@H](C(N([C@@H]([C@@H](C)CC)[C@H](OC)CC(N1CCC[C@@]1([H])[C@H](OC)[C@@H](C)C(N[C@H](C(O)=O)CC2=CC=CC=C2)=O)=O)C)=O)C(C)C)=O.Cl
分子式C39H66ClN5O8
分子量768.42
溶解度DMSO: 27 mg/mL (35.14 mM and warming)
储存条件Store at -20°C,unstable in solution, ready to use.
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

MMAF hydrochloride (Monomethylauristatin F Hydrochloride) is an antitubulin agent that inhibit cell division; inhibits H3397 cell growth with an IC50 of 105 nM. IC50: 119 nM (Cytotoxicity, Karpas 299 cell), 105 nM (Cytotoxicity, H3396 cell), 257 nM (Cytotoxicity, 786-O cell), 200 nM (Cytotoxicity, Caki-1, cell)[1]

MMAF shows in vitro cytotoxicity against a panel of cell lines. The IC50 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-MMAF4 is an average of over 2200-fold more potent than free MMAF and is active on all the CD30-positive cell lines tested[1].

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[1].

[1]. Doronina SO, et al. Enhanced activity of monomethylauristatin F through monoclonal antibody delivery: effects of linker technology on efficacy and toxicity. Bioconjug Chem. 2006 Jan-Feb;17(1):114-24.