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MMAF

现货
Catalog No.
B3270
抗有丝分裂/抗微管蛋白/抗肿瘤剂
组合的产品项目
规格价格库存 数量
5mg
¥ 2,500.00
现货
10mg
¥ 4,200.00
现货
25mg
¥ 9,000.00
现货

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Background

MMAF is a highly potent antimitotic agent [1].

MMAF is an auristatin F (AF) derivative and is used as an antimitotic drug in the form of antibody drug conjugates (ADCs). It is reported that both the N-terminal monomethylvaline and the C-terminal carboxyl group of MMAF can be attached to the linker. Dipeptide linkers used for the attachment of MMAF to mAbs result in conjugates pronounced and potent activities against an array of tumor types. In the in vitro cytotoxicity assays, the ADC generated by attaching MMAF to the 1F6 mAb shows a potent inhibition to the cell viability with IC50 values of 10ng/ml, 8ng/ml, and 123ng/ml in 786-O, Caki-1 and L428 cell lines, respectively. Moreover, it is reported that the dipeptide linker attached to MMAF with C-terminal amino acids could modulate the efficacy, potency, and tolerability. The manipulation of the C-terminal peptide sequence leads to the improved potency, specificity and therapeutic windows of the conjugates [1].

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt731.96
Cas No.745017-94-1
FormulaC39H65N5O8
Solubility≥36.6mg/mL in DMSO
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
SDFDownload SDF
Canonical SMILESCCC(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
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

试验操作

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.

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