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MMAE-d8
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MMAE-d8图片
CAS NO:2070009-72-0
包装与价格:
包装价格(元)
1mg电议
5mg (1mg x 5)电议
10mg (1mg x 10)电议

产品介绍
D8-MMAE (D8-Monomethyl auristatin E) 是氘代标记的 MMAE。MMAE 是一种 tubulin 抑制剂,抑制有丝分裂。
Cas No.2070009-72-0
别名Monomethyl auristatin E-d8; Deuterated labeled MMAE
分子式C39H59D8N5O7
分子量726.03
溶解度DMSO : 100 mg/mL (137.74 mM; Need ultrasonic)
储存条件Store at -20°C,unstable in solution, ready to use.
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

D8-MMAE (D8-Monomethyl auristatin E) is a deuterated labeled MMAE, a potent mitotic inhibitor and a tubulin inhibitor.

Antibody-drug conjugates (ADC) comprise targeting antibodies armed with potent small-molecule payloads. ADCs are generated to target different receptors on the anaplastic large cell lymphoma line L-82, but delivered the same cytotoxic payload (monomethyl auristatin E, MMAE), and the intracellular concentration of released MMAE correlated with in vitro ADC-mediated cytotoxicity independent of target expression or drug:antibody ratios. LC-MS is used to measure the concentration of MMAE in a parallel cohort of L-82 tumors with an identical treatment regimen. Although tumor volume is not different among treatment groups 3 days after dose, the intratumoral MMAE measurement reveals two patterns. First, intratumoral MMAE concentration increases proportionally to the ADC dose, which correspondes to stronger antitumor activity. Second, the intratumoral MMAE concentration obtained from treatment with both cOKT9-vcMMAE and cAC10-vcMMAE is similar at each dose, consistent with the observation that tumor responded similarly to these two ADCs[1].

Intratumoral MMAE concentrations consistently correlates with the extent of tumor growth inhibition in tumor xenograft models. IHC analysis reveals that nonbinding control-treated tumors consist of both CD30+ and CD30-cells, presumably because they do not kill either CD30+ or CD30- Karpas 299 cells. Only CD30- cells are found in cAC10-vcMMAF-treated tumors, illustrating that cAC10-vcMMAF eliminates most CD30+ cells. Interestingly, the two tumors that relapses from cAC10-vcMMAE treatment are also found to be CD30- by the end of study, indicating a small fraction of CD30- cells might have escaped from bystander killing in these two remaining tumors[1].

[1]. Li F, et al. Intracellular Released Payload Influences Potency and Bystander-Killing Effects of Antibody-Drug Conjugates in Preclinical Models. Cancer Res. 2016 May 1;76(9):2710-9.