|4-((S)-2-((S)-2-(6-(2,5-二氧代-2,5-二氢-1H-吡咯-1-基)己酰胺)-3-甲基丁酰胺)-5-脲基戊酰胺)苄基((S)-1-(((S)-1-(((3R,4S,5S)-1-((S)-2-((1R,2R)-3-(((1S,2R)-1-羟基-1-苯丙烷-2-基)氨基)-1-甲氧基-2-甲基-3-氧代丙基）吡咯烷-1-基)-3-甲氧基-5-甲基-1-氧代庚-4-基)(甲基)氨基)-3-甲基-1-氧代丁烷-2-基)氨基)-3-甲基-1-氧代丁烷-2-基)(甲基)氨基甲酸酯|CsnPharm

CAS No.: 646502-53-6

VcMMAE/VcMMAE,用于偶联抗体 Catalog No. CSN16143

Synonyms: MC-Val-Cit-PAB-MMAE;mc-vc-PAB-MMAE;Vedotin

Vc-MMAE is used in ADCs.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Vc-MMAE is a derivate of the antimitotic agent MMAE which has been already linked with the linker dipeptide, valine-citrulline (vc). Vc-MMAE can be directly linked to a monoclonal antibody (MAB) which directs it to the cancer cells. The MMAE part acts as the payload of the ADC. The dipeptide valine-citrulline can be cleaved by lysosome. Thereby, the link between the payload and the monoclonal antibody will cleave and the antimitotic agent MMAE can be released into the cells^[1]. Through combination with specific monoclonal antibody through specific linker, for example, the ADC cAC10-vcMMAE, the cytotoxicity and selectivity of MMAE was significantly enhanced. Intravenous injection with cAC10-vcMMAE at dose of 1mg/kg induced complete, durable tumor regression in the Karpas 299 ALCL model^[2].
临床研究
NCT号适应症或疾病临床期招募状态预计完成时间地点
NCT03274492 Diffuse Large B-Cell Lymphoma Phase 3 Recruiting April 15, 2023 -
参考文献

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03274492	Diffuse Large B-Cell Lymphoma	Phase 3	Recruiting	April 15, 2023	-

[1] Zhao H, Gulesserian S, et al. A Potential Mechanism for ADC-Induced Neutropenia: Role of Neutrophils in Their Own Demise. Mol Cancer Ther. 2017 Sep;16(9):1866-1876.
[2] Francisco JA, Cerveny CG, et al. cAC10-vcMMAE, an anti-CD30-monomethyl auristatin E conjugate with potent and selective antitumor activity. Blood. 2003 Aug 15;102(4):1458-65. Epub 2003 Apr 24.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 0.7595 mL
- 3.7976 mL
- 7.5952 mL
- 5 mM
- 0.1519 mL
- 0.7595 mL
- 1.5190 mL
- 10 mM
- 0.0760 mL
- 0.3798 mL
- 0.7595 mL

技术信息

CAS号

646502-53-6

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C68H105N11O15

运输

蓝冰

分子量

1316.63

别名

MC-Val-Cit-PAB-MMAE;mc-vc-PAB-MMAE;Vedotin;MMAE Vc linker;MMAE antibody conjugate

溶解度

DMSO	98.0 mg/mL (74.4 mM)
Water	Insoluble
Ethanol	100.0 mg/mL (76.0 mM)

动物实验配方

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VcMMAE/VcMMAE,用于偶联抗体 Catalog No. CSN16143

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