VcMMAE

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Chemical Structure| 646502-53-6 同义名 : mc-vc-PAB-MMAE;MC-Val-Cit-PAB-MMAE;MMAE Vc linker, MMAE antibody conjugate;Vedotin
CAS号 : 646502-53-6
货号 : A153774
分子式 : C68H105N11O15
纯度 : 99%+
分子量 : 1316.626
MDL号 : MFCD25372036
存储条件:

Pure form Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 55 mg/mL(41.77 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

无水乙醇: 45 mg/mL(34.18 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

动物实验配方:
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

0.76mL

0.15mL

0.08mL

3.80mL

0.76mL

0.38mL

7.60mL

1.52mL

0.76mL

参考文献

[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.