Monomethyl auristatin E的生物活性
Monomethyl auristatin E (MMAE) is a hot topic in Antibody-drug conjugates (ADCs) studies. It is an antimitotic agent which inhibits cell division by blocking the polymerisation of tubulin.
IC50 Value: N/A
Target: ADCs cytotoxin; Microtubule/Tubulin
For example VcMMAE, an antibody-drug conjugate (ADC) with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc). Antibody-drug conjugates (ADCs) are designed to combine the exquisite specificity of antibodies to target tumor antigens with the cytotoxic potency of chemotherapeutic drugs. In vivo studies demonstrated that the peptide-linked conjugates induced regressions and cures of established tumor xenografts with therapeutic indices as high as 60-fold. These conjugates illustrate the importance of linker technology, drug potency and conjugation methodology in developing safe and efficacious mAb-drug conjugates for cancer therapy.
分子量 |
717.98 |
储存条件 |
参考CoA中推荐的条件进行储存。 |
分子式 |
C39H67N5O7 |
CAS号 |
474645-27-7 |
溶剂/溶解度 |
DMSO > 100 mg/ml |
备注:
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