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Fmoc-Val-Cit-PAB-PNP {[allProObj[0].p_purity_real_show]}

货号:A157658

Fmoc-Val-Cit-PAB-PNP is a linker for ADC through cleaveage by catepsin B only present in lysosome at Val-Cit site, thus making ACD payload be released only in the cell.

Fmoc-Val-Cit-PAB-PNP 化学结构 CAS号:863971-53-3
Fmoc-Val-Cit-PAB-PNP 化学结构
CAS号:863971-53-3
Fmoc-Val-Cit-PAB-PNP 3D分子结构
CAS号:863971-53-3
Fmoc-Val-Cit-PAB-PNP 化学结构 CAS号:863971-53-3
Fmoc-Val-Cit-PAB-PNP 3D分子结构 CAS号:863971-53-3
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Fmoc-Val-Cit-PAB-PNP 纯度/质量文件 产品仅供科研

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Fmoc-Val-Cit-PAB-PNP 生物活性

描述 Fmoc-Val-Cit-PAB-PNP serves as a cleavable linker in antibody-drug conjugate (ADC) synthesis, offering plasma stability on par with non-cleavable linkers[1].[2].[3].
体内研究

The stability of the Fmoc-Val-Cit-PAB-PNP linker in mice is deemed crucial for conducting effective efficacy and safety studies in rodent models, serving as a foundational step in the preclinical phase of ADC development programs[3].

Moreover, the site of conjugation significantly influences the stability of the VC-PABC linker in mouse plasma. There's a positive correlation between the stability of this linker and the cytotoxic potency of the corresponding ADC, both in vitro and in vivo, highlighting the importance of linker design in ADC efficacy[3].

体外研究

This linker includes a peptide sequence susceptible to degradation by lysosomal enzymes[1].

The enzyme Cathepsin B in the lysosome specifically targets and cleaves the peptide bond between Cit-PAB within dipeptide linkers composed of Valine (Val)-citrulline (Cit) and p-aminobenzylalcohol (PAB). This process enables the release of a drug covalently attached to PAB via carbamate bonds, following the peptide bond's cleavage between Cit-PAB, a mechanism exploited in the development of ADCs[2].

Fmoc-Val-Cit-PAB-PNP 参考文献

[1]Dubowchik GM, et al. Cathepsin B-labile dipeptide linkers for lysosomal release of doxorubicin from internalizing immunoconjugates: model studies of enzymatic drug release and antigen-specific in vitro anticancer activity. Bioconjug Chem. 2002 Jul-Aug;13(4):855-69.

[2]Yoneda Y, et al. A cell-penetrating peptidic GRP78 ligand for tumor cell-specific prodrug therapy. Bioorg Med Chem Lett. 2008 Mar 1;18(5):1632-6.

[3]Dorywalska M, et al. Effect of attachment site on stability of cleavable antibody drug conjugates. Bioconjug Chem. 2015 Apr 15;26(4):650-9.

Fmoc-Val-Cit-PAB-PNP 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.30mL

0.26mL

0.13mL

6.52mL

1.30mL

0.65mL

13.04mL

2.61mL

1.30mL

Fmoc-Val-Cit-PAB-PNP 技术信息

CAS号863971-53-3
分子式C40H42N6O10
分子量 766.796
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,2-8°C

溶解度

DMSO: 40 mg/mL(52.17 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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