MMAF
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
MMAF是一种强效的抗有丝分裂剂[1].
MMAF是一种auristatin F(AF)衍生物,以抗体药物偶联物(ADCs)的形式作为抗有丝分裂药物使用.据报道,MMAF的N端monomethylvaline 和C端羧基都可以与接头连接.二肽接头用于MMAF和mAbs连接产生偶联物,其对一系列肿瘤类型产生较强的活性.在体外细胞毒性实验中,MMAF与1F6 mAb连接形成的ADC对细胞活力显示出强的抑制作用,对786-O\Caki-1和L428细胞系的 IC50值分别为10 ng/ml\8 ng/ml和123 ng/ml.此外,据报道,将MMAF与二肽接头的C端氨基酸连接可以调节功效\效力和耐受性.对C-末端肽序列进行改造可改进偶联物的效力\特异性和治疗窗[1].
参考文献:
[1] Doronina SO, Bovee TD, Meyer DW, Miyamoto JB, Anderson ME, Morris-Tilden CA, Senter PD. Novel peptide linkers for highly potent antibody-auristatin conjugate. Bioconjug Chem. 2008 Oct;19(10):1960-3.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 731.96 |
Cas No. | 745017-94-1 |
Formula | C39H65N5O8 |
Solubility | ≥36.6 mg/mL in DMSO; ≥2.62 mg/mL in H2O with gentle warming and ultrasonic; ≥17.2 mg/mL in EtOH |
Chemical Name | (2S)-2-[[(2R,3R)-3-methoxy-3-[(2S)-1-[(3R,5S)-3-methoxy-5-methyl-4-[methyl-[(2S)-3-methyl-2-[[(2S)-3-methyl-2-(methylamino)butanoyl]amino]butanoyl]amino]heptanoyl]pyrrolidin-2-yl]-2-methylpropanoyl]amino]-3-phenylpropanoic acid |
SDF | Download SDF |
Canonical SMILES | CCC(C)C(C(CC(=O)N1CCCC1C(C(C)C(=O)NC(CC2=CC=CC=C2)C(=O)O)OC)OC)N(C)C(=O)C(C(C)C)NC(=O)C(C(C)C)NC |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
786-O、Caki-1和L428细胞 |
制备方法 |
在DMSO中的溶解度大于36.6 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
反应条件 |
96小时 |
实验结果 |
在786-O、Caki-1和L428细胞中,连接MMAF的1F6mAb有效抑制细胞活力,其IC50值分别为10 ng/mL、8 ng/mL和123 ng/mL。 |
动物实验 [1]: | |
动物模型 |
携带786-O RCC异种移植瘤的小鼠 |
给药剂量 |
1或3 mg/kg;腹腔注射 |
实验结果 |
携带786-O RCC异种移植瘤的小鼠中,1F6-Val-Cit-PABC-MMAF比AMAsn-(D)Lys-1F6和AW-Met-(D)Lys-1F6的作用低至少3倍。此外,与AMAsn-(D)Lys-1F6和AW-Met-(D)Lys-1F6相比,1F6-Val-Cit-PABC-MMAF具有较低的耐受性。 |
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。 |
References: [1]. Doronina SO, Bovee TD, Meyer DW, Miyamoto JB, Anderson ME, Morris-Tilden CA, Senter PD. Novel peptide linkers for highly potent antibody-auristatin conjugate. Bioconjug Chem. 2008 Oct;19(10):1960-3. |
质量控制和MSDS
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