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).
性状
Solid
IC50 & Target[1][2]
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. 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. has not independently confirmed the accuracy of these methods. They are for reference only.
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. has not independently confirmed the accuracy of these methods. They are for reference only.
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。
参考文献
[1]. Okeley, et al. Intracellular Activation of SGN-35, a Potent Anti-CD30 Antibody-Drug Conjugate. Clinical Cancer Research (2010), 16(3), 888-897.[2]. Lisa Buckel, et al. Tumor radiosensitization by monomethyl auristatin E: mechanism of action and targeted delivery. Cancer Res. 2015 Apr 1;75(7):1376-87.
溶解度数据
In Vitro: DMSO : ≥ 54 mg/mL (41.01 mM)H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)