DM4-SPDP

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DM4-SPDP 

DM4-SPDP 是由 linker SPDP 和 毒性分子 DM4 连接而成的，可用来制备抗体偶联药物。DM4 是抑制细胞分裂的抗微管蛋剂。SPDP 是一种短链交联剂，可通过 NHS-酯和吡啶基二硫醇反应性基团与半胱氨酸巯基形成可降解 (cleavable) 的 (可还原的) 二硫键，实现胺与巯基的结合。

DM4-SPDP

DM4-SPDP Chemical Structure

CAS No. : 2245698-48-8

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生物活性

DM4-SPDP is a drug-linker conjugate composed of a potent antitubulin agent DM4 and a linker SMCC to make antibody drug conjugate[1]. SPDP is a short-chain crosslinker for amine-to-sulfhydryl conjugation via NHS-ester and pyridyldithiol reactive groups that form cleavable (reducible) disulfide bonds with cysteine sulfhydryls[2][3].

IC50 & Target[1]

Maytansinoids

 

分子量

981.57

Formula

C45H61ClN4O14S2
CAS 号

2245698-48-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Tang R, et al. P-gp activity is a critical resistance factor against AVE9633 and DM4 cytotoxicity in leukaemia cell lines, but not a major mechanism of chemoresistance in cells from acute myeloid leukaemia patients. BMC Cancer. 2009 Jun 23;9:199.

    [2]. Lobedanz S et al. A periplasmic coiled-coil interface underlying TolC recruitment and the assembly of bacterial drug effluxpumps. Proc Natl Acad Sci U S A, 2007 Mar 13, 104(11):4612-7.

    [3]. Karumuthil-Melethil S et al. Dendritic cell-directed CTLA-4 engagement during pancreatic beta cell antigen presentation delays type 1diabetes. J Immunol 2010 Jun 15, 184(12):6695-708.

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