linker-payload

Lys-SMCC-DM1 (Lys-Nε-MCC-DM1) 是一种靶向人表皮生长因子受体2 (HER2) 的 ADC，作为 T-DM1 的活性代谢产物含有微管蛋白聚合抑制剂 DM1，可抑制微管蛋白聚合，常用于乳腺癌的研究。

Thailanstatin A 是真核 RNA 剪接抑制剂，IC50为650 nM，通过非共价结合到剪接体的 U2 snRNA 亚复合物的 SF3b 亚单位发挥作用。Thailanstatin A 对多种癌细胞系的抑制显示 nM 级别的 IC50。它与 Trastuzumab 上的赖氨酸结合，可产生“无连接子” ADC。

ABBV-969 Payload (Br-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT) 是一种药物-连接子偶联物，用于抗体药物偶联物（ADCs）合成。该载荷含有拓扑异构酶 I 抑制剂分子及化学连接子，可与抗 c-Met 抗体偶联，从而生成具有靶向抗癌活性的 ABBV-969 ADCs。

m-PEG4-Br is a cleavable ADC linker used in the synthesis of an antibody-drug conjugate (ADC) for Trastuzumab. It is positioned distally from the monomethyl auristatin E (MMAE) payload, resulting in an ADC with modified hydrophilicity, antigen binding, and in vivo characteristics.

DBCO-(PEG2-VC-PAB-MMAE)2 consists of Monomethyl auristatin E (MMAE), a toxin payload in antibody-drug conjugate [1], conjugated to the cleavable linker DBCO-(PEG2-VC-PAB)2. MMAE, a potent tubulin inhibitor, serves as the cytotoxic component in this formulation.

DBCO-PEG4-SS-TCO is a cleavable 4-unit polyethylene glycol (PEG) linker essential for the synthesis of antibody-drug conjugates (ADCs)[1]. It plays a crucial role in connecting the drug payload to the antibody, enabling targeted drug delivery.

DBCO-(PEG)3-VC-PAB-MMAE is a chemical compound where monomethyl auristatin E (MMAE), a potent tubulin inhibitor acting as a toxin payload in antibody-drug conjugates, is conjugated to a DBCO-(PEG)3-vc-PAB linker.

Mal-Phe-C4-VC-PAB-MMAE is a chemical compound resulting from the conjugation of monomethyl auristatin E (MMAE), a potent tubulin inhibitor serving as a toxin payload in antibody-drug conjugates, with a Mal-Phe-C4-VC-PAB linker.

Mc-MMAD是保护基团Maleimidocaproyl(Mc)修饰的MMAD(Monomethyl auristatin D)。MMAD是一种高效的tubulin微管蛋白抑制剂，能抑制癌细胞增殖，常用作ADC合成中的毒性有效载荷。

NAMPT inhibitor-linker 1, a drug-linker conjugate for ADC, integrates an NAMPT inhibitor (as a payload) with a linker. In the formulation of ADC-3, it pairs with an anti-c-Kit monoclonal antibody, demonstrating strong efficacy against c-Kit expressing cell lines, specifically GIST-T1 and NCI-H526, where it exhibits IC50 values of <3 pM and 9 pM, respectively.

NAMPT inhibitor-linker 2, a drug-linker conjugate for antibody-drug conjugates (ADCs), comprises an NAMPT inhibitor payload and a linker. When combined with an anti-c-Kit monoclonal antibody to form ADC-4, it demonstrates potent efficacy against c-Kit expressing cell lines, including GIST-T1 and NCI-H526, with IC50 values of <7 pM and 40 pM, respectively.

PC Mal-NHS carbonate ester is a cleavable linker specifically designed for the synthesis of antibody-drug conjugates (ADCs)[1]. This chemical compound plays a crucial role in facilitating the conjugation of drugs to antibodies, enabling targeted delivery and enhanced efficacy of therapeutic agents. Its unique carbonate ester structure allows for efficient cleavage in the targeted environment, ensuring the controlled release of the drug payload. Its application in ADC synthesis highlights its importance in the development of innovative and targeted cancer therapies.

SPDB-DM4 is a drug-linker conjugate designed for antibody-drug conjugate (ADC) applications, employing the maytansine-based payload DM4 (a tubulin inhibitor) connected through a SPDB linker. This compound demonstrates significant anti-tumor efficacy.

Sulfo-SPDB-DM4 is a drug-linker conjugate designed for antibody-drug conjugates (ADCs) that employs the maytansine-based payload (DM4, an antitubulin agent) connected through the sulfo-SPDB linker.

Mal-Toxophore 作为一种药物-连接子复合物，广泛应用于 ADC 合成中。其主要有效载荷为NAMPT抑制剂。

APL-1092 (Mal-Exo-EEVC-Exatecan) 作为一种药物-Linker 偶联物，主要应用于 ADC 合成，其结构由 Exatecan (ADC payload) 和 linker 组成。

Mal-PEG4-Val-Cit-PAB-MMAE是抗体偶联活性分子ADC的linker-payload部分，由可降解的ADC linker和微管蛋白抑制剂MMAE组成。

MC-Val-Cit-PAB-Sunitinib 是由有效载荷Sunitinib与连接子组成的化合物。MC-Val-Cit-PAB-Sunitinib 适用于合成 HR97-Sunitinib。

CTT2274 是 MMAE 的前药，由前列腺特异性膜抗原 (PSMA) 结合支架、biphenyl基序、pH 敏感的 phosphoramidate 连接子和 MMAE 载荷组成。CTT2274 选择性结合 PSMA 并递送 MMAE，可抑制前列腺癌。

PNU-EDA 是抗体偶联活性分子 ADC 的一部分。由可裂解的 ADC linker (EDA) 和有效载荷 PNU159682 偶联而成。PNU-EDA 可用于合成 ADC 化合物。

C-lock-GGFG-DXd 是一种硫醇反应型药物连接剂，GGFG是一种可酶解的肽，进入病灶之后可以使有效载荷 DXd 释放发挥作用，C-lock-GGFG-DXd 常用于抗体-药物偶联物（ADC）的合成。

C-lock-GGFG-Exatecan 是一种硫醇反应型药物连接剂，GGFG是一种可酶解的肽，进入病灶之后可以使有效载荷 Exatecan 释放发挥作用，C-lock-GGFG-Exatecan 常用于抗体-药物偶联物（ADC）的合成。

MC-VC-PAB-Exatecan 是抗体偶联活性分子 ADC 的一部分。由可裂解的 ADC linker (MC-VC-PAB) 和有效载荷 Exatecan 偶联而成。MC-VC-PAB-Exatecan 常用于合成 ADC 化合物。

Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27) 是一种用于ADC的活性分子-偶联物，由ADC接头 Mal-N(Me)-C6-N(Me) 和有效的ADC细胞毒素 PNU-159682 组成。此化合物通过组织蛋白酶 B 裂解接头选择性地将有效载荷递送到表达 CD46 的细胞中，释放 PNU-159682，从而诱导 DNA 损伤和细胞凋亡 (apoptosis)。在非小细胞肺癌 (NSCLC) 和结直肠癌 (CRC) 异种移植 (PDX) 模型中，Mal-N(Me)-C6-N(Me)-PNU-159682 表现出持久的肿瘤消退效果。