VcMMAE是抗体偶联药物的一部分，具有抗癌活性，它由 MM

VcMMAE  (Synonyms: MC-Val-Cit-PAB-MMAE; mc-vc-PAB-MMAE)

VcMMAE (mc-vc-PAB-MMAE) 是抗体偶联药物的一部分 (drug-linker conjugate for ADC)，具有抗癌活性，它由 MMAE (一种 tubulin 抑制剂) 和 valine-citrulline (vc) 连接而成。

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生物活性    
VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).

IC50 & Target    
Auristatin


体外研究
(In Vitro)    
Monomethyl auristatin E (MMAE) is efficiently released from SGN-35 within CD30+ cancer cells and, due to its membrane permeability, is able to exert cytotoxic activity on bystander cells[1]. MMAE sensitized colorectal and pancreatic cancer cells to IR in a schedule and dose dependent manner correlating with mitotic arrest. Radiosensitization is evidenced by decreased clonogenic survival and increased DNA double strand breaks in irradiated cells[2].

体内研究
(In Vivo)    
Monomethyl auristatin E (MMAE) in combination with IR results in tumor growth delay, tumor-targeted ACPP-cRGD-MMAE with IR produces a more robust and significantly prolonged tumor regression in xenograft models[2].

分子量    
1316.63

性状    
Solid

Formula    
C68H105N11O15

CAS 号    
646502-53-6

运输条件    
Room temperature in continental US; may vary elsewhere.

储存方式    
-20°C, sealed storage, away from moisture and light

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。

溶解性数据    
In Vitro: 
DMSO : ≥ 54 mg/mL (41.01 mM)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

* "≥" means soluble, but saturation unknown.

配制储备液    
浓度溶剂体积质量    1 mg    5 mg    10 mg
1 mM    0.7595 mL    3.7976 mL    7.5951 mL
5 mM    0.1519 mL    0.7595 mL    1.5190 mL
10 mM    0.0760 mL    0.3798 mL    0.7595 mL
*
请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

In Vivo:
1.
VcMMAE is dissolved in DMSO and then diluted with 0.9% NaCl[3].