ADC Cytotoxin

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).

Hemiasterlin is a cytotoxic peptide that acts by inducing mitotic arrest and abnormal spindle formation.

Exatecan analogue 1 (Icp-3) 是 Exatecan 的类似物，可用于合成抗体-药物偶联物 (ADCs)。

Exatecanintermediate 9 作为合成Exatecan的关键中间体,在制备ADC时常用作毒素成分 (ADC Cytotoxin).Exatecan (DX-8951) 本身则是一种有效的 DNA 拓扑异构酶 I (topoisomerase I) 抑制剂,具有IC50值为2.2 μM.

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

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)。

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。

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。

Piericidin A是一种天然来源的线粒体NADH-泛醌氧化还原酶（复合物 I）抑制剂。Piericidin A通过抑制 NADH-泛醌还原酶活性干扰电子传递链，从而抑制线粒体呼吸，中表现出一定的神经毒性作用。Piericidin A具有潜在的群体感应抑制活性和抗菌、抗肿瘤及杀虫等生物活性。

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

Bac5(1-25) 为抗菌肽Bac5的N端片段，该肽源自牛富含脯氨酸。

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。

STINGagonist-35 (Compound 1a) 是干扰素基因刺激剂 (STING) 的激动剂，激活野生型 STING 和突变型 STING (R232H)，激活率分别为 99% 和 92%。STINGagonist-35 有潜力成为 ADC 药物的有效载荷。

7-Ethylcamptothecin 是一种喜树碱类似物。其中喜树碱是一种细胞毒性生物碱，从喜树中分离出得到，对 L1210 白血病和 Walker 256 癌肉瘤模型具有很强的抗肿瘤活性。

Methotrexate disodium 是一种叶酸类似物代谢抑制剂，具有免疫抑制剂和抗肿瘤特性，用于类风湿关节炎和研究多种癌症。

Aldoxorubicin has effective antitumor activities in various cancer cell lines and in murine tumor models. Aldoxorubicin is an albumin-binding prodrug of Doxorubicin (DNA topoisomerase II inhibitors).

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。

Ansamitocin p-3 (Maytansinol isobutyrate) 是一种微管抑制剂，对微管蛋白聚合的 IC50 为 3.4 μM。

MMAF (MonoMethyl auristatin F) 是一种抗有丝分裂剂，通过阻断微管蛋白的聚合来抑制细胞分裂，用作抗肿瘤药物和抗体偶联药物的细胞毒性成分。

SG2057 (DRG16) 是一种含有戊二氧基键的 PBD 二聚体，该键选择性地结合DNA 小沟中的序列，形成 DNA 链间和链内交联加合物。SG2057 是一种高效抗肿瘤剂。

Polyketomycin is a tetracyclic quinone glycoside antibiotic isolated from Streptomyces sp. or Streptomyces diastatochromogenes, has antibacterial, anticancer, antimalarial activities.

ε-Amanitin is a cyclic peptide obtained from various mushroom species. It exhibits a strong affinity for RNA polymerase II and effectively inhibits its activity.

Dolastatin 10 (DLS 10) 是一种多肽，可以抑制微管蛋白聚合，显示除抗有丝分裂的活性。

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。

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.

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

Tubulysin IM-2 is an ADC Cytotoxin and tubulin binder used as anti-microtubule toxins .

(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。

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].

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。

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。

Duocarmycin DM free base是一种具有细胞毒性的抗肿瘤抗生素和DNA 烷化剂。它通过与 DNA 小沟结合并对腺嘌呤进行序列特异性烷基化来诱导 DNA 断裂，常作为抗体偶联药物 (ADC) 的高效载荷 (Payload) 用于实体瘤研究。

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)。

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

Aminohexylgeldanamycin (AHGDM), a derivative of Geldanamycin, is a highly effective inhibitor of HSP90. It exhibits considerable antiangiogenic and antitumor properties[1].

MMAF Hydrochloride is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as Vorsetuzumab mafodotin and SGN-CD19A. MMAF Hydrochloride is an effective tubulin polymerization inhibitor and is used as an antitumor compound.