ADC Cytotoxin

Top1 inhibitor 1 is a potent inhibitor of human topoisomerase I (Top1)(IC50: 29 nM).

DGN462 is an effective DNA alkylating agent with anti-tumor activity, as in acute myeloid leukemia (AML). DGN462 can be used as a cytotoxic component of antibody-drug conjugates (ADCs).

10-Methoxycamptothecin 是分离自喜树的喜树碱衍生物，具有高抗癌特性。通过对 2774 细胞系的抗肿瘤活性测定，发现它比 10-羟基喜树碱的细胞毒性更高。

Luisol A 是一种芳香族四醇，是链霉菌属的河口海洋放线菌的主要代谢产物。Luisol A 是一种蒽醌抗生素类似物，是 ADC 细胞毒素 (ADC Cytotoxin)。

Glucocorticoid receptoragonist-2 (compound 21) 作为一种糖皮质激素受体激动剂，具有 6.6 nM 的 IC50 值，主要用于抗炎 ADC 分子的合成。同时，它也是 ABBV-3373 的活性对照物。

Tubulysin E is a natural product isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis, and is a highly cytotoxic peptide.

TAM470 是一种新型的细胞溶素，可抑制微管蛋白聚集和微管解聚。TAM470 可作为有效载荷分子用于合成 OMTX705，OMTX705 是一种具有抗肿瘤活性的FAP 靶向抗体偶联活性分子 (ADCs)。

Hygrolidin is a macrocyclic lactone originally isolated from S. hygroscopicus. It inhibits proliferation of a variety of cancer cell lines, including DLD-1 colon cancer, LNCaP prostate cancer, and K562 leukemia cells (IC50s = 2.9, 5.2, and 33 ng/ml, respectively). Hygrolidin induces the expression and levels of p21 in DLD-1 cells, but not WI-38 fibroblasts, and leads to cell accumulation in the G1 and S phases without inducing apoptosis. It has antiparasitic activity against T. cruzi, L. donovani, and T. b. brucei but also induces cytotoxicity in HepG2 cells (IC50s = 1.1, 72.5, 77, and 24.5 nM, respectively).

Nucleoside Derivatives - Fluoro-modified nucleosides; 5-Modified pyrimidine nucleosides; 3'-Deoxy nucleosides

Duocarmycin MB can be used against multi-drug resistant cell lines. Duocarmycin MB is an antibody drug conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove.

TH1338 是具有口服活性喜树碱的衍生物，具有潜在的抗癌活性。TH1338 具有显著的血脑屏障透过性和细胞毒性，可用于研究癌症。

DM4 (Ravtansine)可用于制备抗体药物偶联物，是抗微管蛋白剂。 它抑制细胞分裂。

Duocarmycin A, an antitumor antibiotic, is a DNA alkylator and efficiently alkylates adenine N3 at the 3′ end of AT-rich sequences in the DNA. Duocarmycin A, as a chemotherapeutic agent, results in HLC-2 cells typically apoptotic changes.

PBD-monoamide, a modified pyrrolobenzodiazepine (PBD) dimer, functions as an ADC cytotoxin. It is utilized in synthesizing DHES0815A (an HER2 ADC) and possesses DNA-binding activity that reduces cell viability [1].

Glucocorticoid receptoragonist-3 (Preparation 6) 属于糖皮质激素受体激动剂类化合物。

Dox-btn2 是 Doxorubicin 的生物素化衍生物，在 3'-NH2 与阿霉素的偶联点上有生物素标记。Dox-btn2 可用于细胞成像。Doxorubicin 主要积累在细胞核中，而 Dox-btn2 主要位于细胞质中。

MMAF-methyl ester 为一种ADC毒素.

MYX1715，作为N-肉豆蔻酰转移酶（NMT）的抑制剂，其KD值为0.09 nM。该化合物能有效抑制LU0884和LU2511细胞系的增殖，其IC50分别为44 nM和9 nM。在小鼠模型中，MYX1715对神经母细胞瘤和胃癌展示了显著的抗肿瘤活性，并可作为ADC毒素使用。

SC209intermediate-2 (Compound A9) 作为一种ADC Linker，是用于合成ADC细胞毒素SC209的关键中间体。

Glucocorticoid Receptor Agonist-4 (Compound Preparation 5) serves as an agonist for glucocorticoid receptors and can be conjugated with TNF-α antibodies, facilitating research into autoimmune and inflammatory diseases [1].

DMEA-PNU-159682 (molecule D12) dichloroacetate, 作为一种ADC细胞毒素分子，由肝微粒体的新霉素代谢产物 (MMDX) 与高效的ADC细胞毒素PNU-159682组成。

BTKdegrader-1 (compound 1) 作为一种针对布鲁顿氏酪氨酸激酶 (BTK) 的双功能降解剂，能够与 CD79b 结合，展现出其抗肿瘤的功效。

NMS-P528是一种Duocarmycin衍生物，可用作ADC有效负载 (ADC payload)，并可用于合成NMS-P945。

Exatecan-amide-bicyclo[1.1.1]pentan-1-ol (Compound 79) 为一种基于 exatecan 的衍生物，常见于药物缀合物的有效载体中。该化合物在抑制多种肿瘤细胞系方面展示出优异的活性。

Dov-Val-Dil-OH 是 ADC 毒素的一种.

Exatecan Intermediate 7 为Exatecan的中间体.Exatecan (DX-8951) 作为一种抑制DNA拓扑异构酶I (topoisomerase I) 的化合物,具有IC50值2.2 μM (0.975 μg/mL),主要用于癌症研究.此中间体还可用于合成抗体-药物偶联物 (Antibody-Drug Conjugates (ADCs)).

Antitumor agent-203 (compound 26) 是 Exatecan(DX-8951) 的衍生物，能够作为 ADC Cytotoxin，用于制备抗体-药物偶联物 (ADC)。

Aeruginosin 865, isolated from terrestrial cyanobacterium Nostoc sp . Luke ová 30/93, is the first aeruginosin-type peptide containing both a fatty acid and a carbohydrate moiety. Aeruginosin 865 inhibits translocation of NF-kB to the nucleus. Aeruginosin 865 has anti-inflammatory effect

(4-NH2)-Exatecan是一种拓扑异构酶抑制剂，具有潜在的抗癌活性，可用于合成抗体药物共轭物（ADC）。

Duocarmycin is a DNA minor groove binding alkylating agent and explored as drug–antibody conjugates (ADCs) . Duocarmycin is based on its characteristic curved indole structure and a spirocyclopropylcyclohexadienone electrophile to act anticancer activity.

C-11 is a tubulin inhibitor and acts as an ADC cytotoxin with cytotoxicity for carcinoma cell lines.

DMEA-PNU-159682 (molecule D12) is an ADC cytotoxin molecule that includes neomycin (MMDX) metabolites from liver microsomes and the effective ADC cytotoxin PNU-159682.

Tubulysin I is a natural product isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis, and is a highly cytotoxic peptide. Tubulysin I is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to c

DC1 is an ADC cytotoxin, similar to the small groove-binding DNA alkylating agent CC-1065. DC1 can be used to synthesize antibody-drug conjugates targeted to the treatment of cancer. DC1Sme is a DC1 derivative with IC50 values of Ramos, Namalwa, HL60 / s

Dxd (OQM5SD32BQ) 是一种有效的DNA 拓扑异构酶 I 抑制剂（IC50= 0.31 μM）。Dxd用作HER2靶向ADC 的偶联药物。

(S)-Seco-Duocarmycin SA 是一种 DNA 烷化剂，也是具有高效抗肿瘤活性的抗生素，可用于合成 ADC 化合物。