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MCMMAE

MCMMAE
上海 更新日期:2024-02-02

上海芮珊医药科技有限公司

VIP8年
联系人:邱先生
手机:17321237488 拨打
邮箱:kevin@resuperpharmtech.com

产品详情:

中文名称:
MCMMAE
英文名称:
MCMMAE
CAS号:
863971-24-8
品牌:
RSP
产地:
上海
保存条件:
0-10度
纯度规格:
95%

Monomethyl auristatin E (MMAE), a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate; Mc-MMAE is a protective group (maleimidocaproyl) -conjugated MMAE.
IC50 value:
Target:
Effective antibody-drug conjugates (ADC) combine high drug-linker stability in circulation and efficient intratumoral release of drug. Conjugation of monomethyl auristatin E (MMAE) to the anti-CD30 monoclonal antibody (mAb), cAC10, produced a selective and potent ADC against CD30+ anaplastic large cell lymphoma and Hodgkin's disease models. This ADC, cAC10-valine-citrulline-MMAE, uses a protease-sensitive dipeptide linker designed to release MMAE by lysosomal cathepsin B in target cells but maintain a stable linkage and attenuate drug potency in circulation. To evaluate ADC stability in vivo, we developed methods for measuring drug/mAb ratios at progressive times in plasma from ADC-treated mice and nonhuman primates. Anti-idiotype mAb permitted the capture and quantitation of mAb cAC10, whereas antidrug mAb and MMAE-conjugated horseradish peroxidase reporter provided quantitative detection of conjugated drug following its in vitro release by cathepsin B. These data were validated by an alternative ELISA using anti-idiotype and anti-MMAE mAbs for capture and detection, respectively. Both methods differentiated ADC with variable levels of drug loading and were subsequently applied to stability studies in severe combined immunodeficient mice and cynomolgus monkeys. Evaluation of ADC from mouse circulation showed the linker half-life to be ~144 hours (6.0 days), significantly greater than that reported for disulfide- or hydrazone-linked ADCs in mice or human trials. In cynomolgus monkey, the apparent linker half-life was ~230 hours (9.6 days), suggesting that the drug-linker will be highly stable in humans. These data represent the longest reported drug-linker half-life to date and provide the basis for the pronounced specificity and antitumor activity of cAC10-valine-citrulline-MMAE.

公司简介

上海芮珊医药科技有限公司是以医药中间体和原料药研发为中心,集产品生产、推广等各个环节为一体的新兴高科技产业公司。公司致力于以化学原料药中间体、生物医药技术为核心的生产、研发、销售、贸易一体化服务,代理原料药杂质,参比制剂, 生物药等前沿产品。 我们本着“平等互利、真诚合作、恪守信誉、协同共赢”的宗旨,以良好的企业形象,优质的服务,高效的工作,可靠的信誉,竭诚欢迎与各界合作,用我们的真诚和汗水,以求发展,共创未来

成立日期 (8年)
注册资本 50W
员工人数 1-10人
年营业额 ¥ 100万以内
经营模式 贸易,试剂,定制
主营行业 中间体,医药原料

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