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Monomethyl auristatin E

CAS号

474645-27-7

分子式

C39H67N5O7

主要靶点

Microtubule Associated|Apoptosis

仅限科研使用

Cat No : CM00853

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Synonyms

Inhibitor|MMAE|Monomethyl auristatin E|MicrotubuleAssociated|microtubule|Microtubule/Tubulin|Microtubule Associated|Vedotin|SGD 1010|SGD1010|SGD-1010|一甲基澳瑞他汀E|inhibit|Apoptosis|ADC Cytotoxin|ADCCytotoxin|ADC Payload

验证数据展示

  • CAS No.: 474645-27-7

    Monomethyl auristatin E
    CAS#: 474645-27-7

产品信息

CAS号 474645-27-7
分子式 C39H67N5O7
主要靶点 Microtubule Associated|Apoptosis
主要通路 凋亡|抗体-药物偶联物/ADC 相关|细胞骨架
分子量 717.98
纯度 99.66%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 Inhibitor|MMAE|Monomethyl auristatin E|MicrotubuleAssociated|microtubule|Microtubule/Tubulin|Microtubule Associated|Vedotin|SGD 1010|SGD1010|SGD-1010|一甲基澳瑞他汀E|inhibit|Apoptosis|ADC Cytotoxin|ADCCytotoxin|ADC Payload

体内活性

在Karpas 299 ALCL模型中，cAC10-vcMonomethyl auristatin E（1 mg/kg，i.v.）引起完全且持久的肿瘤消退，而自由Monomethyl auristatin E（0.36 mg/kg）未显示出可检测的抗肿瘤活性。[1] 在NHL小鼠异种移植模型中，anti–CD79b-vcMonomethyl auristatin E（7 mg/kg，p.o.）显著导致持续的完全肿瘤缓解。[2]

体外活性

当与cAC10结合时，Monomethyl auristatin E在CD30+细胞中表现出选择性的细胞毒性，并通过诱导凋亡来引起G2/M期生长停滞和细胞死亡。[1] 当与抗CD79b抗体结合时，抗CD79b-vcMonomethyl auristatin E对体外的大量NHL细胞系具有非常强大和广泛的活性。[2] 当与抗HER2抗体结合时，hertuzumab-vc-Monomethyl auristatin E也能有效地被内化，并强力地杀死过表达HER2的肿瘤细胞。[3]

溶解度

DMSO:71.8 mg/mL (100 mM)

细胞实验

Cytotoxicity is measured using Alamar Blue dye reduction assay according to the manufacturer's directions. Briefly, a 40% solution (wt/vol) of Alamar Blue is freshly prepared in complete media just before cultures are added. Ninety-two hours after drug exposure, Alamar Blue solution is added to cells to constitute 10% culture volume. Cells are incubated for 4 hours, and dye reduction is measured on a Fusion HT fluorescent plate reader (Packard Instruments, Meriden, CT). (Only for Reference)

参考文献

1.Francisco JA, et al. Blood. 2003, 102(4), 1458-1465.
2.Dornan D, et al. Blood. 2009, 114(13), 2721-2729.
3.Yao X, et al. Breast Cancer Res Treat. 2015, 153(1), 123-133.

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