MC-Val-Cit-PAB

A peptide linker molecule

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库存: 现货

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价格

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数量
250mg

￥937.00

750.00

- +
500mg

￥1412.00

1130.00

- +
1g

￥2125.00

1700.00

- +
2g

￥3362.00

2690.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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货号: ajce57372
CAS: 159857-80-4
别名:
分子式: C28H40N6O7
分子量: 572.65
纯度: >98%
溶解度: DMSO: ≥ 52 mg/mL (90.81 mM)
储存: 4°C, protect from light, stored under nitrogen
库存: 现货

Background

Mc-Val-Cit-PAB is a peptide linker molecule used in the synthesis of antibody-drug conjugates (ADCs).¹ It contains a maleimidocaproyl (Mc) group that can be conjugated to an antibody and a p-aminobenzyl (PAB) spacer that allows the peptide to be linked to active compounds, such as anticancer agents. Mc-Val-Cit-PAB is cleaved in vivo by cathepsin B, a protease highly expressed in cancer cells, which confers specificity of the ADC to cancer cells. Upon cleavage by cathepsin B, the active compound is released at the target site. Mc-Val-Cit-PAB has been used in the synthesis of an ADC containing the tubulin polymerization inhibitor KGP05. It has also been used as a precursor in the synthesis of Mc-Val-Cit-PABC-PNP .²

1.Mondal, D., Ford, J., and Pinney, K.G.Improved methodology for the synthesis of a cathepsin B cleavable dipeptide linker, widely used in antibody-drug conjugate researchTetrahedron Lett.59(40)3594-3599(2018) 2.Dubowchik, G.M., Firestone, R.A., Padilla, L., 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 activityBioconjug. Chem.13(4)855-869(2002)