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MMAE-d8

MMAE-d8

产品编号 T10948   CAS 2070009-72-0
别名: D8-MMAE, D8-Monomethyl auristatin E

D8-MMAE (D8-Monomethyl auristatin E) is an effective mitotic inhibitor and tubulin inhibitor, deuterated MMAE.

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MMAE-d8 Chemical Structure
MMAE-d8, CAS 2070009-72-0
规格 价格/CNY 货期 数量
25 mg 待询 10-14周
50 mg 待询 10-14周
100 mg 待询 10-14周

MMAE-d8 的其他形式现货产品:

Monomethyl auristatin E
其他形式的 MMAE-d8:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: MMAE-d8 (T10948)
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该分子属于定制产品。陶术拥有优秀的合成团队,经验和能力,可以为您提供高性价比的产品。但由于客观因素,研发中会存在小概率合成不成功的情况,还请理解,如您有任何问题,欢迎咨询,我们将竭诚为您服务。
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 D8-MMAE (D8-Monomethyl auristatin E) is an effective mitotic inhibitor and tubulin inhibitor, deuterated MMAE.
体外活性 Antibody-drug conjugates (ADC) contain targeted antibodies with effective small molecule payloads. The ADC is produced against different receptors on the anaplastic large cell lymphoma L-82 line, but delivers the same cytotoxic payload (monomethyl auristatin E, MMAE). ADC-mediated cytotoxicity is not related to target expression or drug: antibody ratio. LC-MS was used to measure the concentration of MMAE in the L-82 tumor parallel cohort by the same treatment protocol. Although there was no difference in tumor volume between the treatment groups 3 days after administration, intratumoral MMAE measurements showed two patterns. First, the MMAE concentration in the tumor increases in proportion to the ADC dose, which corresponds to stronger antitumor activity. Second, intra-tumor MMAE concentrations obtained after treatment with cOKT9-vcMMAE and cAC10-vcMMAE were similar at each dose, which is consistent with the observation that tumors responded similarly to these two ADCs.
体内活性 In tumor xenograft models, the MMAE concentration in the tumor is always correlated with the degree of tumor growth inhibition. IHC analysis showed that tumors that were not combined with control treatment consisted of CD30 + and CD30 cells, presumably because they did not kill CD30 + or CD30- Karpas 299 cells. Only CD30-cells were found in tumors treated with cAC10-vcMMAF, indicating that cAC10-vcMMAF eliminated most CD30 + cells. Interestingly, at the end of the study, two tumors recurring from the treatment of cAC10-vcMMAE were also found to be CD30-, indicating that in the remaining two tumors, a small portion of CD30-cells may have escaped bystanders Kill.
别名 D8-MMAE, D8-Monomethyl auristatin E
分子量 726.03
分子式 C39H59D8N5O7
CAS No. 2070009-72-0

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 100 mg/mL (137.74 mM), Sonication is recommended.

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.3774 mL 6.8868 mL 13.7735 mL 34.4338 mL
5 mM 0.2755 mL 1.3774 mL 2.7547 mL 6.8868 mL
10 mM 0.1377 mL 0.6887 mL 1.3774 mL 3.4434 mL
20 mM 0.0689 mL 0.3443 mL 0.6887 mL 1.7217 mL
50 mM 0.0275 mL 0.1377 mL 0.2755 mL 0.6887 mL
100 mM 0.0138 mL 0.0689 mL 0.1377 mL 0.3443 mL

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TargetMol Library Books参考文献

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.

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体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

MMAE-d8 2070009-72-0 Others MMAE-d-8 MMAE d8 D8-MMAE MMAEd8 D8-Monomethyl auristatin E Inhibitor inhibitor inhibit

 

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