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。

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。

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。

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。

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。

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)。

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。

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

Mc-VC-PAB-SN38 由可降解 (cleavable) 的 ADC linker (Mc-VC-PAB) 和 SN38 组成，属于抗体偶联活性分子的一部分，常用来合成靶向作用位点的抗体偶联活性分子 (ADC)。

Gly3-VC-PAB-MMAE is a chemical compound comprised of a cleavable antibody-drug conjugate (ADC) linker, Gly3-VC-PAB, and a potent inhibitor of tubulin, MMAE. It is utilized in the synthesis of ADCs.

DGN549-L is a DNA alkylator that facilitates antibody conjugation at lysine residues, making it suitable for antibody-drug conjugate (ADC) synthesis.

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。

SMP-33693为一种抗体-药物偶联物（Antibody-Drug Conjugates (ADCs)），其有效载荷（payload）稳定性高，显示出对卵巢癌、胃癌及乳腺癌肿瘤的体内抑制作用。

MC-SN38 is a drug-linker conjugate that pairs the potent microtubule-disrupting agent SN38 with a non-cleavable MC linker, designed for use in antibody drug conjugates (ADCs). SN38, the active metabolite of the Topoisomerase I inhibitor Irinotecan, works by inhibiting DNA synthesis and inducing DNA single-strand breaks.

ST8155AA1为一种抗体偶联药物（ADCs）成分，载有HDAC抑制剂并连接物，展现出对抗肿瘤的活性。

Gly-Mal-Gly-Gly-Phe-Gly-amide-methylcyclopropane-Exatecan 适合用作抗体药物偶联物（ADC）的合成工艺。

Biotin-PEG7-Maleimide是一种能与硫醇基(SH)反应的生物素化试剂，适用于作为ADC药物连接偶联剂(Drug-Linker Conjugates for ADC)。

MC-DM1 is a drug-linker conjugate composed of a potent microtubule-disrupting agent DM1 and a linker MC to make antibody drug conjugate (ADC).

MP-PEG4-Val-Lys-Gly-7-MAD-MDCPT is a Camptothecin-linker. MP-PEG4-Val-Lys-Gly-7-MAD-MDCPT is a drug-linker conjugate for antibody-drug conjugate (ADC).

MC-VC-PAB-MMAD为一种抗体-活性分子偶联物，连接了微管抑制剂MMAD与可降解的ADC linker MC-VC-PAB。

β-Glucuronide-dPBD-PEG5-NH2 TFA 是一种通过β-葡糖苷酸与pyrrolobenzodiazepine形成的二聚体，能够与异戊二烯化的抗体结合，生成抗体-活性分子偶联物(ADC) cIRCR201-dPBD。该化合物中的β-葡糖苷酸键作为可降解的ADC Linker，有助于减少副作用。β-Glucuronide-dPBD-PEG5-NH2 TFA 作为cIRCR201-dPBD的前体，显示出能诱导细胞凋亡(apoptosis)和阻滞细胞周期，具备抗肿瘤活性。

Glucocorticoid receptoragonist-1 Ala-Ala-Mal (化合物 88) 是一种糖皮质激素，是糖皮质激素受体激动剂。Glucocorticoid receptoragonist-1 Ala-Ala-Mal 可与Adalimumab 偶联制备ADC。

SuO-Glu-Val-Cit-PAB-MMAE is a chemical compound comprising a cleavable ADC linker, SuO-Glu-Val-Cit-PAB, and a potent tubulin inhibitor known as MMAE. It is utilized in the synthesis of antibody-drug conjugates (ADCs).

TLR7 8 agonist 4 hydroxy-PEG10-acid (compound 9) is a drug-linker conjugate employed in antibody-drug conjugates (ADC). This compound exhibits remarkable antitumor activity by utilizing TLR7 8 agonist 4, which acts as a potent activator of TLR7 8. The TLR7 8 agonist 4 is linked to hydroxy-PEG10-acid, the ADC linker, via a cleavable bond. Overall, it demonstrates promising pharmaceutical potential in the context of ADC-based therapeutics.

Azido-PEG4-Val-Cit-PAB-MMAE is a drug-linker conjugate for antibody-drug conjugates (ADCs), comprising the anti-mitotic agent monomethyl auristatin E (MMAE, a tubulin inhibitor), connected through the cleavable linker Azido-PEG4-Val-Cit-PAB-OH.

LP-6是一种ADC药物-连接子偶联物 (Drug-Linker Conjugates for ADC)，用于ADC的合成，由Eg5抑制剂和连接子组成。

MC-Gly-Gly-Phe-Gly-GABA-Exatecan ADC 是一种药物连接子偶联物，其包含的拓扑异构酶Exatecan具有22 μM 的IC50值。该化合物在体外和体内对多种抗体显示出细胞毒性及抗肿瘤效果。

Glucocorticoid receptoragonist-4 Ala-Ala-Mal (化合物 Preparation 9) 是一种缀合物，它将抗人 TNFα 抗体与糖皮质激素受体激动剂 (GC) 结合。此化合物主要用于自身免疫性疾病和炎症性疾病的研究。

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.

SC-VC-PAB-MMAE is a potent antitumor drug-linker conjugate for antibody-drug conjugates (ADCs), comprising the anti-mitotic agent monomethyl auristatin E (MMAE, a tubulin inhibitor) connected through the cleavable linker SC-VC-PAB[1].

MC-VC-PABC-Aur0101 is a potent anticancer drug-linker conjugate designed for Antibody-Drug Conjugates (ADCs), comprising Aur0101, an auristatin microtubule inhibitor, connected through the MC-VC-PABC linker to enhance antitumor efficacy.

Daunorubicinol, a potent antitumor drug-linker conjugate for antibody-drug conjugate (ADC) applications, utilizes Aur0101 (DNA Topoisomerase II inhibitor) connected through the ADC linker[1].

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.

AcLys-PABC-VC-Aur0101 is a drug-linker conjugate for anti-CXCR4 ADC with potent antitumor activity, comprising the auristatin microtubule inhibitor Aur0101, connected through the cleavable linker AcLys-PABC-VC[1].

Vc-seco-DUBA is a drug-linker conjugate for ADC with potent antitumor activity by using DUBA (DNA alkylating agent), linked via the ADC linker Vc-seco[1].

MC-Val-Cit-PAB-Auristatin E is an antibody-drug conjugate (ADC) linker compound featuring Auristatin E, a potent cytotoxic tubulin modifier, connected through the MC-Val-Cit-PAB linker, exhibiting significant antitumor activity.

Mal-PEG4-VC-PAB-DMEA-PNU-159682 is a drug-linker conjugate designed for antibody-drug conjugate (ADC) therapy. It combines the ADC linker, Mal-PEG4-VC-PAB, with the potent ADC cytotoxin, DMEA-PNU-159682. The cytotoxin, DMEA-PNU-159682, is derived from metabolites of nemorubicin (MMDX) found in liver microsomes, as well as the ADC cytotoxin PNU-159682[1].

DBCO-PEG4-VA-PBD is a cleavable 4-unit PEG ADC linker utilized in antibody-drug conjugate (ADC) synthesis [1].

MC-Alkyl-Hydrazine Modified MMAF is a potent antitumor drug-linker conjugate for ADC, incorporating Modified MMAF, a tubulin inhibitor, through a noncleavable MC-Alkyl-Hydrazine linkage[1].

Mal-C6-α-Amanitin is a drug-linker conjugate for ADC with potent antitumor activity by using α-Amanitin (an RNA polymerase II inhibitor), linked via the ADC linker Mal-C6.

CL2E-SN-38 TFA为一抗体-SN-38稳定偶联体，属抗体药物偶联物(ADC)范畴。SN-38是Irinotecan活性代谢产物，源自喜树碱，作为拓扑异构酶I的抑制剂。

Mc-Val-Cit-PAB-Gefitinibchloride是一种担载EGFR酪氨酸激酶抑制剂Gefitinib的ADC活性分子连接子偶联物，由Gefitinib和专为ADC设计的连接子Mc-Val-Cit-PAB构成。

Mal-PEG8-Val-Cit-PAB-MMAF 是一种用于抗体药物偶联体 (ADC) 的药物-连接物复合体 (drug-linker conjugate for ADC)。该化合物由一个可降解的 ADC linker 以及有效的微管蛋白抑制剂 MMAE 组成。

Azide-PEG4-VC-PAB-Doxorubicin 为链接剂 Azide-PEG4-VC-PAB 与毒性分子 Doxorubicin 结合形成，适用于抗体药物偶联物（ADCs）的制备。