drug-linker conjugates for adc

SMCC-DM1 (DM1-SMCC) 是一种药物-接头偶联物，由有效的微管破坏剂 DM1 和接头 SMCC 组成，用于制备抗体药物偶联物。

Deruxtecan 是一种 ADC 药物-接头偶联物，由 DX-8951 (DXd) 的衍生物和马来酰亚胺-GGFG 肽接头组成，用于合成 DS-8201 和 U3-1402。

Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) 是保护基团 (马来酰亚氨基己酰) 与 MMAE 共轭连接得到的化合物。它是微管蛋白抑制剂，可用于偶联抗体。

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。

Vipivotide tetraxetan (PSMA-617) 是一种高效的前列腺特异性膜抗原抑制剂，其Ki 值为 0.37 nM。

Vc-MMAD 由 linker (Val-Cit) 和微管抑制剂 MMAD 组成。Vc-MMAD 可用于偶联抗体。

VCMMAE (mc-vc-PAB-MMAE) 是一种用于 ADC 的药物-接头偶联物，具有抗癌活性，它由 MMAE 和 Vc 连接而成。

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。

McMMAF 是一种保护基团共轭的 MMAF。它是一种具有马来酰亚胺基己酰基接头（MC 接头）的 MMAF 衍生物， MMAF 是一种有效的微管蛋白聚合抑制剂。它可与抗体或其他蛋白质或生物聚合物结合。

CL2A-SN-38 由CL2A链接子和抗癌化合物SN-38 组成，可在肿瘤细胞内和肿瘤微环境中递送活性活性分子，通常会与抗体制成具有生物活性的抗体偶联活性分子 (ADC)。

Fmoc-PEA 是一种可降解的抗体偶联药物 (ADC)的linker。

DSS Crosslinker 是一种不可切割的 ADC 连接剂，用于合成抗体-药物偶联物。

MC-Gly-Gly-Phe 是一种用于抗体-药物偶联物的可切割接头。

Phe-Lys(Trt)-PAB 是一种组织蛋白酶可裂解的 ADC 接头，用于合成抗体-药物偶联物。

MC-Val-Cit-PABC-PNP 是一种组织蛋白酶可裂解的 ADC 肽接头，可用于合成抗体偶联药物。

Fmoc-Val-Ala-PAB-OH (Fmoc-Val-Ala-PAB) 是一种有用的接头，可用于制备用于靶向药物递送的抗体-药物偶联物。它还用于合成带有溶酶体可切割接头的 RGD 拟肽-紫杉醇缀合物。

TCO-PEG4-NHS ester 是一种属于 PEG 类的 PROTAC 连接桥。TCO-PEG4-NHS ester 可用于合成一系列 PROTAC 分子。TCO-PEG4-NHS ester 是一种可降解 (cleavable) 且可用于抗体活性分子结合物 (ADCs) 的合成 ADC 连接桥。

CCK2R Ligand-Linker Conjugate 1 is a hydrophilic peptide linker that conjugates to the cytotoxic antimicrotubule agents Desacetyl Vinblastine Hydrazide (DAVBH) and Tubulysin B Hydrazide (TubBH) as ligand-linker conjugates[1].

Fmoc-Val-Cit-PAB-MMAE 由 ADC 接头 (Fmoc-Val-Cit-PAB) 和强效微管蛋白抑制剂 (MMAE) 组成。 它是一种用于 ADC 的药物-接头偶联物。

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-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-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.

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.

Acetylene-linker-Val-Cit-PABC-MMAE (LCB14-0602) is a drug-linker conjugate for antibody-drug conjugates (ADCs) that combines the ADC linker (Acetylene-linker-Val-Cit-PABC) with the potent tubulin inhibitor MMAE.

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].

N3-PEG3-vc-PAB-MMAE, a drug-linker conjugate designed for Antibody-Drug Conjugates (ADC), features the integration of monomethyl auristatin E (MMAE), a tubulin inhibitor, via a 3-unit polyethylene glycol (PEG) linker. This compound demonstrates significant antitumor activity.

SPP-DM1, a drug-linker conjugate for antibody-drug conjugates (ADC), demonstrates potent antitumor activity. It comprises DM1 (a potent microtubule-disrupting agent) connected through the ADC linker SPP[1].

PEG4-aminooxy-MMAF is a drug-linker conjugate designed for antibody-drug conjugates (ADC) that exhibits potent antitumor activity. It incorporates MMAF, a powerful antitubulin agent, connected through a non-cleavable PEG4 linker[1].

MMAE-SMCC is a drug-linker conjugate designed for antibody-drug conjugates (ADC). It consists of MMAE, a potent inhibitor of mitosis and tubulin, and SMCC, a linker that facilitates the development of ADCs.

MC-Sq-Cit-PAB-Gefitinib is a potent antitumor drug-linker conjugate for Antibody-Drug Conjugates (ADC), utilizing Gefitinib—an EGFR tyrosine kinase inhibitor—connected through the MC-Sq-Cit-PAB ADC linker.

Mal-C2-Gly3-EDA-PNU-159682, a drug-linker conjugate for antibody-drug conjugates (ADC), combines the cleavable ADC linker Mal-C2-Gly3-EDA with the potent ADC cytotoxin PNU-159682.

SPB is a potent anti-inflammatory drug-linker conjugate for Antibody-Drug Conjugates (ADC), utilizing Xanthotoxol connected through the ADC linker.

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].

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].

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].

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].

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.

MC-Val-Cit-PAB-rifabutin is a drug-linker conjugate designed for antibody-drug conjugates (ADC), featuring the potent antitumor agent rifabutin (a DNA-dependent RNA polymerase inhibitor) connected through the MC-Val-Cit-PAB ADC linker. This configuration endows it with significant antitumor activity.

MC-Val-Cit-PAB-vinblastine is a potent antitumor drug-linker conjugate for Antibody-Drug Conjugates (ADC), featuring vinblastine (a microtubule protein inhibitor) connected through the MC-Val-Cit-PAB ADC linker.

DM4-SMCC, a non-cleavable drug-linker conjugate for antibody-drug conjugates (ADC), leverages the antitumor efficacy of DM4 (an antitubulin agent) through attachment with the SMCC linker, exhibiting antitumor activity[1].

MC-Val-Cit-PAB-Retapamulin is a drug-linker conjugate for antibody-drug conjugates (ADC) that exhibits potent antitumor activity. This compound utilizes Retapamulin, a ribosome inhibitor, connected through the ADC linker MC-Val-Cit-PAB.

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

AcLysValCit-PABC-DMAE-SW-163D is a drug-linker conjugate for antibody-drug conjugates (ADCs), featuring a natural bis-intercalator, SW-163D, attached through an AcLysValCitPABC-DMAE linker[1].

7-O-(Cbz-N-amido-PEG4)-paclitaxel is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.

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.

MC-Val-Cit-PAB-MMAF is an antibody-drug conjugate (ADC) component that exhibits antitumor properties through the action of the tubulin inhibitor, monomethyl auristatin F (MMAF), which is connected by a cathepsin-cleavable linker, MC-Val-Cit-PAB.

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].

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.