| Molecular Weight: | 731.96 |
| Formula: | C39H65N5O8 |
| Purity: | ≥95% |
| CAS#: | 745017-94-1 |
| Solubility: | DMSO up to 20 mM |
| Chemical Name: | (S)-2-((2R,3R)-3-((S)-1-((3R,4S,5S)-4-((S)-N,3-dimethyl-2-((S)-3-methyl-2-(methylamino)butanamido)butanamido)-3-methoxy-5-methylheptanoyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropanamido)-3-phenylpropanoic acid |
| Storage: | Powder: -20oC 1 year |
Monomethyl auristatin F (MMAF) is an anti-mitotic agent that inhibits cell division by blocking the polymerization of tubulin. It is a new auristatin derivative ith a charged C-terminal phenylalanine residue that attenuates its cytotoxic activity compared to its uncharged counterpart MMAE. Because of its super toxicity, it cannot be used as a drug itself. It is linked to a monoclonal antibody (mAb) that directs it to the cancer cells. The linker to the monoclonal antibody is stable in extracellular fluid, but is cleaved by cathepsin once the conjugate has entered a tumor cell, thus activating the anti-mitotic mechanism.
Reference:
- 1. Smith LM, et al. Potent cytotoxicity of an auristatin-containing antibody-drug conjugate targeting melanoma cells expressing melanotransferrin/p97. (2006) Mol Cancer Ther. 5(6):1474-82
- 2. Doronina, SO, et al. Enhanced activity of monomethylauristatin F through monoclonal antibody delivery: effects of linker technology on efficacy and toxicity. (2006) Bioconjug Chem, 17(1):114-24.
- 3. Oflazoglu E, et al. Potent anticarcinoma activity of the humanized anti-CD70 antibody h1F6 conjugated to the tubulin inhibitor auristatin via an uncleavable linker. (2008) Clin Cancer Res. 14(19):6171-80.
- 4. Nilsson R, et al. Toxicity-reducing potential of extracorporeal affinity adsorption treatment in combination with the auristatin-conjugated monoclonal antibody BR96 in a syngeneic rat tumor model. (2010) Cancer 116(4 Suppl):1033-42.
- 5. http://en.wikipedia.org/wiki/Monomethyl_auristatin_E
MMAF_spec.pdf
MMAF_MSDS.pdfProducts are for research use only. Not for human use.
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就是蛋白质分子的小片断
是氨基酸形成的
求助各位前辈,我最近在合成的化合物水溶性很好,非常好,以至于可以随便溶解在水里,它的六氟磷酸盐也可以随意溶解在水里(大于50uM),细胞成像实验显示它根本进不去细胞,求问有没有啥方法包裹一下让它进去?我搜了一下文献,感觉多数是把脂溶性特别好的东西包裹一下弄进去的,也许是搜索姿势不对没找到我需要的答案,**点拨啊!!!
如题,之前没做过药代,老师给了一个600+Da的五肽,想测下药代动参数,看文献推荐上述两种方法,但是不知道选哪种更好,lcms前处理会不会影响小肽。
有机的是有机化合物的简称,它指的是含碳化合物.
但是,有四大类常见物质一般不作为有机物处理:
1、碳的氧化物,如CO和CO2.
2、碳酸及其盐,如CaCO3.
3、金属碳化物,如CaC2.
4、拟卤素及其化合物,如(CN)2与KSCN.
水的化学式为H2O,它不含有碳元素,故不是有机物.
但若所描述的水不是化学意义的水,而是自然界存在的天然水,那么,水中会溶有一定量的有机物.

