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MMAE-d8 (Synonyms: Monomethyl auristatin E-d8; Deuterated labeled MMAE) 纯度: 99.29%
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。
MMAE-d8 Chemical Structure
CAS No. : 2070009-72-0
规格 | 价格 | 是否有货 | 数量 |
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1 mg | ¥11000 | In-stock | |
5 mg (1 mg x 5) | ¥25000 | In-stock | |
10 mg (1 mg x 10) | ¥47300 | In-stock |
* Please select Quantity before adding items.
生物活性 |
D8-MMAE (D8-Monomethyl auristatin E) is a deuterated labeled MMAE, a potent mitotic inhibitor and a tubulin inhibitor. |
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IC50 & Target |
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体外研究 (In Vitro) |
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]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
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]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
726.03 |
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Formula |
C39H59D8N5O7 |
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CAS 号 |
2070009-72-0 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
*该产品在溶液状态不稳定,建议您现用现配,即刻使用。 |
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溶解性数据 |
In Vitro:
DMSO : 100 mg/mL (137.74 mM; Need ultrasonic) 配制储备液
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请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液;该产品在溶液状态不稳定,建议您现用现配,即刻使用。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Kinase Assay [1] |
Cell pellets are collected 24 hours after ADC treatment. Cell count, diameter, and circularity are determined on Vi-Cell Counter. MMAE extraction and quantification method is performed. Briefly, tumors or cell pellets are homogenized with methanol and acetonitrile containing internal standard (d8-MMAE for MMAE detection and 13C-MMAF for MMAF detection). The homogenates are centrifuged at 10,000 rpm to precipitate protein and protein-bound payloads. The supernatant is then subjected to solid phase extraction, and signals of MMAE and MMAF are detected by LC-MS[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only. |
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参考文献 |
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