目录:MedChemExpress LLC>>生化试剂>> PAC | MCE
CAS | 2158322-33-7 | 纯度 | 98.96% |
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分子量 | 1674.93 | 分子式 | C₉₄H₁₀₇N₁₃O₁₆ |
供货周期 | 现货 | 货号 | HY-112100 |
应用领域 | 医疗卫生,化工,生物产业,制药/生物制药 |
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CAS No. : 2158322-33-7
产品活性:PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
研究领域:Vitamin D Related/Nuclear Receptor | PROTAC | Antibody-drug Conjugate/ADC Related
作用靶点:Estrogen Receptor/ERR | PROTAC-Linker Conjugates for PAC
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) .
相关产品:Estradiol hemihydrate | OP-1074 | GSK-4716 | LSD1/ER-IN-1 | Avobenzone | Cholesterol-13C2 | Cholesterol-18O | Diethylstilbestrol | ERB-196 | FLTX1 | Raloxifene hydrochloride | Tamoxifen | Estradiol-d2-1 | Bazedoxifene acetate | FSHR agonist 1 | Estrone sulfate sodium | GNE-502 | β-Estradiol 17-acetate | Enclomiphene | AhR modulator-1 | α-Zearalenol | SNIPER(ER)-87 | ERRα antagonist-2 | Estradiol-d2 | Cholesterol-d7 | PROTAC BRD4 Degrader-5-CO-PEG3-N3 | (Rac)-Hexestrol-d4 | Cholesterol-d | (E)-4-Hydroxytamoxifen
热门产品线:重组蛋白 | 化合物库 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物 | 寡核苷酸 | 抗体 | 点击化学
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