Drug-Linker Conjugates for ADC

DBCO-HS-PEG2-VA-PABC-SG3199 是一种用于 ADC 的药物-连接子偶联物 (drug-linker conjugate for ADC)，该化合物包含基于 SG3199 的 DNA 小沟交联剂和可裂解连接子。此化合物可用于合成 ADCs。

DGN549-C is a novel compound featuring a cleavable ADC (antibody-drug conjugate) linker composed of valine-alanine (va) and a PBD (pyrrolobenzodiazepine) dimer. This compound possesses a unique DNA-alkylating cytotoxic payload, DGN549, which is utilized in the development of ADCs.

MC-Val-Cit-PAB-Indibulin is an antitumor drug-linker conjugate for antibody-drug conjugates (ADCs), featuring the orally active tubulin assembly inhibitor, Indibulin, connected through the MC-Val-Cit-PAB ADC linker. This compound exhibits potent antitumor activity.

MC-betaglucuronide-MMAE-2 是由微管蛋白聚合抑制剂 MMAE 与 ADC linker MC-betaglucuronide 可降解连接组成的抗体-活性分子偶联物部分。

Fmoc-Val-Cit-PAB-Duocarmycin TM is a drug-linker conjugate designed for antibody-drug conjugation (ADC), utilizing the antitumor antibiotic Duocarmycin TM. It is connected through the linker Fmoc-Val-Cit-PAB.

Val-Cit-PAB-MMAF为抗体偶联药物(ADC)活性组分，其结构由ADC linker（肽Val-Cit-PAB）与高效的微管蛋白聚合抑制剂MMAF通过偶联形成。

MC-EVCit-PAB-MMAE (Linker-Payload 11) 作为一种ADC (drug-linker conjugates) 的代表，由具有功能性的ADC linker (MC-EVCit-PAB) 以及作为有效药物负载的微管蛋白聚合抑制剂MMAE组成。

Mal-PEG4-VA-PBD is a drug-linker conjugate for Antibody-Drug Conjugates (ADCs), comprising the antitumor antibiotic Pyrrolobenzodiazepine (PBD), connected through Mal-PEG4-VA.

MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan 是抗体偶联活性分子的一部分 (drug-linker conjugate for ADC)，包含 Exatecan 。Exatecan 是一种 DNA 拓扑异构酶 I (Topoisomerase I) 抑制剂 (IC50=2.2 μM)。

MP-PEG8-Val-Lys-Gly-7-MAD-MDCPT为喜树碱-接头化合物，属于抗体偶联活性分子（drug-linker conjugate for ADC）部分。该化合物在癌症及自身免疫性疾病研究中显示出研究潜力。

ATAC21是一种连接子免疫刺激化合物，它通过含琥珀酰亚胺基团的稳定型马来酰亚胺-PEG4连接子与免疫刺激化合物结合而成。ATAC21能够与SBT-040（抗CD40抗体）结合，形成具有免疫激活作用的偶联物。

Deruxtecananalog 2（示例9 P3）是一种含活性分子-linker的Deruxtecan类似物，由Camptothecin（一种对多种癌症如结直肠癌、乳腺癌、肺癌和卵巢癌具有抗肿瘤活性的Topo I抑制剂）和linker组成，主要用于开发针对EGFR2的抗体药物偶联物（ADC）活性分子。

MC-GGFG-DX8951(MC-GGFG-Exatecan)是一种抗体偶联药物（ADC）的药物-连接子偶联物（drug-linker conjugate）.由强效的DNA拓扑异构酶I抑制剂DX8951、连接子MC和可被蛋白酶降解（cleavable）的肽链GGFG组成，具有抗肿瘤的潜力。

Propargyl-PEG4-GGFG-DXd 作为抗体偶联活性分子（drug-linker conjugate for ADC）的组成部分，整合了一个可降解的ADC linker与 DNAtopoisomerase I 抑制剂 DXd。

Gemcitabine-O-Si(di-iso)-O-Mc, a drug-linker conjugate for Antibody-Drug Conjugates (ADC), exhibits potent antitumor activity. It incorporates Gemcitabine, a pyrimidine nucleoside analog antimetabolite and antineoplastic agent, connected through the ADC linker[1].

Mal-(CH2)5-Val-Cit-PAB-Eribulin is a potent antitumor ADC drug-linker conjugate that utilizes Eribulin, an anti-microtubule agent, connected through the Mal-(CH2)5-Val-Cit-PAB linker.

ST8154AA1为抗体-药物偶联体（ADCs）成分，载有HDAC抑制剂及连接体，表现出抗肿瘤效能。

MAC glucuronide α-hydroxy lactone-linked SN-38 (Topoisomerase I inhibitor) is a stabilized lactone MAC glucuronide α-hydroxy lactone-linked SN-38 drug linker. MAC glucuronide α-hydroxy lactone-linked SN-38 is cytotoxic across L540cy cells and Ramos cells

DBCO-PEG4-Ahx-DM1 is a drug-linker conjugate that combines the microtubulin inhibitor DM1 (mertansine), which is an antibody-conjugatable maytansinoid designed to reduce systemic toxicity and improve tumor-specific delivery, with the linker DBCO-PEG4-Ahx, for the development of antibody drug conjugates (ADCs).

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.

MC-DOXHZN hydrochloride is an albumin-binding prodrug of Doxorubicin. Doxorubicin is a DNA topoisomerase II inhibitor.

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.

DM4-SPDP, a drug-linker conjugate, integrates the antitubulin agent DM4 with the linker SMCC, facilitating the creation of antibody drug conjugates[1]. Additionally, SPDP serves as a short-chain crosslinker enabling amine-to-sulfhydryl conjugation, leveraging NHS-ester and pyridyldithiol groups to establish cleavable (reducible) disulfide bonds with cysteine sulfhydryls[2][3].

DL-01 为 ADC 用途的活性分子-连接子偶联物(drug-linker conjugates for ADC)，适合于 ADC 合成。

Mc-Dexamethasone is a drug-linker conjugate for ADC . Mc-Dexamethasone is made toxin Dexamethasone conjugated to the non-cleavable MC linker. Dexamethasone is a glucocorticoid receptor agonist.

Mal-PEG4-VC-PAB-DMEA-Seco-Duocarmycin SA is an antibody-drug conjugate linker that incorporates the antitumor antibiotic Duocarmycin SA, connected through the Mal-PEG4-VC-PAB-DMEA-Seco linker, for targeted cancer therapy.

SG3199-Val-Ala-PAB为Tesirine合成中间体，该物质作为用于抗体偶联活性分子(ADC)的活性分子-linker连接物，适用于多种癌症研究。

DM1-(PEG)4-DBCO is a drug-linker conjugate that combines the potent microtubulin inhibitor mertansine (DM1) with the DBCO-PEG4-Ahx linker for the development of antibody-drug conjugates (ADCs). This conjugation aims to mitigate the systemic toxicity associated with maytansine while improving tumor-specific delivery, leveraging DM1’s capabilities as an antibody-conjugatable maytansinoid.

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.

MC-VC-PABC-DNA31 is a drug-linker conjugate designed for Antibody-Drug Conjugates (ADC) that demonstrates potent antitumor activity. It employs DNA31, an effective inhibitor of RNA polymerase, connected through the MC-VC-PABC ADC linker.

PB038为一种ADC药物，由可降解的PEG linker及毒素分子依喜替康(Exatecan)构成的偶联物。

MC-Val-Cit-PAB-Exatecan (MC-Val-Cit-PAB-DX8951) 由细胞毒素，topoisomerase I抑制剂DX-8951，和对组织蛋白酶敏感的连接子构成，是抗体偶联药物（ADC）的药物-连接子偶联物，。

Barzuxetan 用于癌症研究。

Ac-Lys-Val-Cit-PABC-MMAE作为一种抗体偶联药物(ADC)的活性分子部分，由ADC连接子（肽 Ac-Lys-Val-Cit-PABC）与微管蛋白聚合抑制剂MMAE经偶联形成。

MC-Val-Cit-PAB-carfilzomib is a potent antitumor drug-linker conjugate for antibody-drug conjugates (ADC), comprising the irreversible proteasome inhibitor carfilzomib, connected through the ADC linker MC-Val-Cit-PAB.

VCP-Eribulin, an Eribulin-based drug for antibody conjugates[1], combines the VCP (ADCs linker) with Eribulin, a distinct microtubule inhibitor used in cancer treatments[2].