分子量 |
1674.93
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CAS RN® |
2158322-33-7
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構造 |
C94H107N13O16
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使用目的 |
PAC comprises an antibody conjugated via a linker to a PROTAC. PAC extracts from patent WO2017201449A1, compound PAC1. PAC is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).IC50 & Target: Estrogen receptor-alpha (ERα)[1]In Vitro: Treatment of HER2 expressing cells with HER2 antibody containing PAC Anti-HER2(Endox-XIAP) results in a marked decreased Estrogen Receptor-alpha (ERα) levels with an IC50 of 132 ng/mL. The PROTAC-Antibody Conjugate (PAC) molecules comprise an antibody conjugated via a linker (L1) to a PROTAC, wherein the PROTAC comprises an ubiquitin E3 ligase binding group (“E3LB”), a linker (“L2”) and a protein binding group (“PB”). The following sections describe the components that comprise the PAC. To obtain a PAC having potent efficacy and a desirable therapeutic index, the following components are provided. 1. Antibody (Ab): The antibody portion of a PAC can target a cell that expresses an antigen whereby the antigen specific PAC is delivered intracellularly to the target cell, typically through endocytosis While PACs that comprise an antibody directed to an antigen that is not found on the cell surface may result in less specific intracellular delivery of the PROTAC portion into the cell, the PAC may still undergo pinocytosis. 2. Linkers (L1): A“linker” (L1) is a bifunctional or multifunctional moiety that can be used to link one or more PROTAC moieties (D) to an antibody (Ab) to form a PAC. In some embodiments, PACs can be prepared using a L1 having reactive functionalities for covalently attaching to the PROTAC and to the antibody. 3. PROTAC(D) [1].
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[注意事項] |
[溶解度表記について]MCH社のWeb及びデータシート等で溶解度が「<1 mg/ml」のように記載されている場合、その化合物はその溶媒に、溶けないまたはわずかに溶けることを意味しています。(この場合、1mg/ml以下の濃度では試験していません。) 「>90mg/mL」のように記載されている場合、その化合物はその溶媒に90mg/ml で溶けたことを示しています。(ただし、最大でどのくらい溶けるかは試験していません。)
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メーカー |
品番 |
包装 |
MCH
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HY-112100
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5 MG
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※表示価格について
当社在庫 |
なし
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納期目安 |
3週間程度
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法規制 |
劇
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保存温度 |
-20℃
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