Network Version
Product Name: | VcMMAE | |
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CAS No.: | 646502-53-6 | |
Cat. No.: | HY-15575 | |
MWt: | 1316.63 | |
Formula: | C68H105N11O15 | |
Purity : | >98% | |
Solubility: | H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble); DMSO : ≥ 54 mg/mL (41.01 mM) | |
Mechanisms: | Target: Cancer | |
Biological Activity: | ||
VcMMAE (mc-vc-PAB-MMAE) is a agent-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). 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]. 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]. |
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