Drug-Linker Conjugates for ADC

OBI-992 drug-linker 是一种由 TOP I 抑制剂 Exatecan 和连接子组成的药物-连接子复合物，在小鼠模型中展示了抗癌活性，并可用于制备 ADC OBI-992。

CL2A-FL118 是一种用于合成 ADC 分子 Sac-CL2A-FL118 的药物-连接子。

2-MSP-5-HA-GGFG-NH-CH2-O-CH2-CO-(5-Cl)-Exatecan 是一种用于 ADC 的药物-linker 偶联物，由 linker 和 Exatecan 组成。

Cys-MC-GGFG-Dxd 是 Cys 和 Deruxtecan 的偶联物。这种化合物是抗体-药物偶联物 (ADC) 中的连接子-毒素结构单元，能够将抗体的 Cys 残基与细胞毒性药物结合。Cys-MC-GGFG-Dxd 在癌症研究中有应用。

Mal-Val-Lys-PAB-MMAE 是一种用于 ADC 的药物-连接子偶联物 (drug-linker conjugate for ADC)，其中包含 ADC linker (Mal-Val-Lys-PAB) 和有效的微管蛋白聚合 (tubulin polymerization) 抑制剂 MMAE。

Mal-PEG2-VCP-Eribulin is a chemotherapeutic compound comprising an antibody-drug conjugate (ADC) linker (Mal-PEG2-VCP) and the microtubule inhibitor Eribulin[1]. This compound uniquely targets microtubules, offering a novel approach to cancer treatment. Eribulin is specifically utilized in creating targeted Eribulin-based drugs for antibody conjugates[1].

HS-(CH2)3CO-L-Ala-D-Ala-L-Ala-NH-CH2-S-(CH2)5-CO-DM 是一种用于抗体偶联药物(ADC)的药物连接体。其中DM代表了maytansinoid组分。

β-Glucuronide-dPBD-PEG5-NH2 是由 β-葡糖苷酸与 pyrrolobenzodiazepine 通过二聚体形成方式连接，并能与异戊二烯化抗体结合形成抗体-活性分子偶联物 (ADC) cIRCR201-dPBD 的化合物。其所含β-葡糖苷酸键为一种可降解 (cleavable) 的 ADC Linker，作为 cIRCR201-dPBD 的前体能有效减少副作用。此外，β-Glucuronide-dPBD-PEG5-NH2 还具备诱导细胞凋亡 (apoptosis) 和阻滞细胞周期的能力，显示出抗肿瘤活性。

DBCO-PEG4-VC-PAB-DMEA-PNU-159682, a drug-linker conjugate for antibody-drug conjugates (ADC), comprises the ADC linker DBCO-PEG4-VC-PAB and the potent ADC cytotoxin DMEA-PNU-159682. The cytotoxin includes metabolites of nemorubicin (MMDX) from liver microsomes and the ADC cytotoxin PNU-159682[1].

TLR7/8 agonist 4hydroxy-PEG6-acid 为ADC药物-连接子偶联物（Drug-Linker Conjugates for ADC）。该合成物结合了TLR7/8 agonist 4与连接子hydroxy-PEG6-acid，专门用于ADC合成。

Mal-VC-PAB-(N-Me-amide-C3)-ADU-S100 triethylamine 是一种免疫刺激物抗体偶联物 (ISAC) 的连接子–payload 小分子，包含STING 激动剂 (ADU- S100) 和一个连接子。Mal-VC-PAB-(N-Me-amide-C3)-ADU-S100 triethylamine 可用于癌症研究。

Val-Cit-PAB-MMAE 是 ADC 的药物-接头偶联物。它包含 ADC 接头（肽 Val-Cit-PAB）和有效的微管蛋白抑制剂 MMAE。

TLR7/8 agonist 4 hydroxy-PEG10-acid hydrochloride (compound 9) is a drug-linker conjugate used in antibody-drug conjugates (ADCs) with high efficacy against tumors. It consists of TLR7/8 agonist 4, a potent TLR7/8 agonist, linked to the ADC linker hydroxy-PEG10-acid which can be cleaved.

Mal-PEG8-Phe-Lys-PAB-Exatecan（化合物15）作为抗体药物偶联物（ADC）的药物连接子部分，由Mal-PEG8-Phe-Lys-PAB这一可降解连接子和毒素分子Exatecan构成。

MAL-di-EG-Val-Cit-PAB-MMAF refers to a chemical compound that comprises the linker (MAL-di-EG-Val-Cit-PAB) and the potent blocker of tubulin polymerization (MMAF, Monomethyl auristatin F)[1].

MC-Sq-Cit-PAB-Dolastatin10 is a potent antitumor drug-linker conjugate for Antibody-Drug Conjugates (ADC), utilizing Dolastatin10 (a tubulin polymerization inhibitor) connected through the MC-Sq-Cit-PAB ADC linker.

Cys-mcMMAD is a drug-linker conjugate for ADC (antibody-drug conjugate) featuring MMAD, a potent tubulin inhibitor.

AmPEG6C2-Aur0131 is a drug-linker conjugate designed for anti-CXCR4 ADC applications, showcasing potent antitumor activity. It incorporates Aur0131, an auristatin-based microtubule inhibitor, connected through the non-cleavable AmPEG6C2 linker.

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.

DM21 is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

MP-PEG8-VA-PABC-PBD Dimer is a drug-linker conjugates for ADC which is used in the treatment of several cancers. PBD Dimer is a DNA alkylating which inhibits DNA replication[1].

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。

MC-vc-PAB-Tubulysin M is a conjugate composed of a cleavable ADC linker (MC-vc-PAB) and the cytotoxic tubulin inhibitor Tubulysin M, which inhibits tubulin polymerization, resulting in cell cycle arrest and apoptosis.

GGFG-amide-glycol-amide-Exatecan(Intermediate 2)为Exatecan衍生物，适用于合成抗体药物偶联物(ADC)。

TCO-PEG4-VC-PAB-MMAE为一种抗体偶联药物（ADC）中的活性药物连接子部分，融合了可降解的ADC连接子（TCO-PEG4-VC-PA）与有效的微管蛋白抑制剂MMAE。

Endo-BCN-PEG4-Val-Cit-PAB-MMAE is a cleavable four-unit polyethylene glycol (PEG) linker, specifically designed for the synthesis of antibody-drug conjugates (ADCs)[1].

Mal-VC-PAB-ABAEP-Azonafide, an ADC (antibody-drug conjugate) linker-drug conjugate, demonstrates potent antitumor activity. It incorporates Azonafide, a cytotoxin, connected through the ADC linker Mal-VC-PAB[1].

Mal-PEG8-Val-Ala-PAB-Exatecan（化合物9b）是一种用于连接抗体与Nectin-4多肽结合的化疗活性分子的ADC linker，适用于癌症研究。

Glucocorticoid receptor agonist-1 phosphate Gly-Glu-Br 为ADC linker，适用于ABBV-154、ABBV-927及ABBV-368或相似化合物的合成。

Doxorubicin-SMCC is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

SN38-PAB-Lys(MMT)-oxydiacetamide-PEG8-N3 是一款用于抗体药物偶联物 (ADC) 合成的化学试剂，由抗癌药物SN38与链接子Lys(MMT)-PAB-oxydiacetamide-PEG8-N3 构成，属于点击化学工具。该化合物含有Azide基团，它可通过铜催化的叠氮-炔点击反应 (CuAAc) 与含Alkyne基团的分子耦合，亦能通过应变促进的炔-叠氮点击反应 (SPAAC) 与含DBCO 或 BCN 基团的分子反应。

Amino-PEG4-Val-Cit-PAB-MMAE is a cleavable tetraethylene glycol (4 unit PEG) antibody-drug conjugate (ADC) linker employed in the synthesis of ADCs[1].

Mal-VC-PAB-DM1, a drug-linker conjugate for antibody-drug conjugates (ADCs), exhibits potent antitumor activity. It incorporates DM1, a potent microtubule-disrupting agent, connected through the ADC linker Mal-VC-PAB [1].

Sulfo-PDBA-DM4 is a drug-linker conjugate for antibody-drug conjugate (ADC) applications, combining the potent tubulin inhibitor DM4 with the gluthatione-cleavable linker Sulfo-PDBA. This configuration harnesses DM4's cytotoxic potential through Sulfo-PDBA's targeted delivery mechanism.

MC-betaglucuronide-MMAE-1 is a potent antitumor drug-linker conjugate for antibody-drug conjugates (ADCs), employing MMAE (a tubulin polymerization inhibitor) connected through the cleavable ADC linker MC-betaglucuronide.

MC-GGFG-AM-(10Me-11F-Camptothecin) 是ZW251合成的Linker-Payload偶联物。ZW251是靶向人GPC3的抗体-活性分子偶联物(ADC)，包括人源化IgG1抗体、喜树碱(camptothecin)类的扑异构酶1抑制剂ZD06519及连接子（马来酰亚胺锚定和甘酰甘酰苯丙酰甘氨酸(GGFG)-氨基甲基(AM)可切割连接体）。该药物对人和食蟹猴GPC3具高亲和力，在表达GPC3的HCC细胞系中快速内化并可对GPC3阴性癌细胞进行旁观者介导杀伤。