ADC Cytotoxin

Doxorubicin（Adriamycin）是一种具有荧光性的蒽环类抗肿瘤抗生素，可抑制Topoisomerase I/II，诱导细胞凋亡和自噬，下调AMPK信号通路，常用于肿瘤化疗，并可用于诱导肾炎和心力衰竭模型。

γ-Amanitin an ADC cytotoxin and isolated from the mushroom. γ-Amanitin inhibits RNA polymerase II and disrupts synthesis of mRNA. γ-Amanitin shows similar effects to α-Amanitin and β-Amanitin.

INX-SM-6适用于靶向输送抗炎药物。它能在PBMCS细胞中抑制LPS引发的IL-1β产生。

SGD-1882 (PBD dimer) 是一种有细胞毒性的偶联剂，是靶向小鼠和人造血干细胞 （HSC） 和急性髓性白血病细胞的载荷。

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.

Seco-Duocarmycin SA is a highly potent DNA alkylator used as an ADC cytotoxin.

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

Dexamethasone acetate monohydrate is an adrenocortical steroid. It is used in the treatment of many conditions, including rheumatic problems, a number of skin diseases, asthma, severe allergies, chronic obstructive lung disease, brain swelling, croup, and antibiotics

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).

alpha-Amanitin (α-Amanitin) 是鹅膏菌中致命的毒素，过肠肝循环和运输系统在体内起作用。alpha-Amanitin 可诱导细胞死亡，可用于合成 ADC。

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。

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.

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.

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。

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。

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

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

Isofistularin-3, as a DNA demethylating agent, induces cell cycle arrest and sensitization to TRAIL in cancer cells. Isofistularin-3 can be used as an ADC cytotoxin.Isofistularin-3 is a direct, DNA-competitive DNMT1 inhibitor, with an IC50 of 13.5 μM.

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。

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

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。

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。

Exatecan-amide-CH2-O-CH2-CH2-OH (Compound 4) 作为Exatecan的衍生物，主要用于癌症及其他细胞增殖性疾病的研究应用。

Exatecan-2-(aminomethoxy)acetamide-Gly-Fmoc 为一种ADC毒素.

(5-Cl)-Exatecan (compound 1-5) 作为一种ADC细胞毒素，主要用于癌症研究。它是一种高效的DNA拓扑异构酶抑制剂。

AXC-879是一种TLR激动剂（EC50：157.2 nM），同时用作一种ADC细胞毒素，用于ADC合成。

Maytansinoid DM4, a thiol-containing maytansine derivative, is a highly potent cytotoxic moiety utilized in ADC applications.

TAM557 is a cytotoxic tubulysin compound suitable for use in enzymatic conjugation reactions [1].

Exatecan-d5(mesylate) 为 Exatecan mesylate 的氘标记版本,主要作为 DNA 拓扑异构酶 I (topoisomerase I) 的抑制剂,其 IC50 值达 0.975 μg/mL.

(R)-Exatecan Intermediate 1 为 Exatecan Intermediate 1 的异构体,属于Exatecan的中间体之一.Exatecan (compound 6) 作为一种喜树碱类的抗癌药物,其机制是通过与DNA相互作用,进而干扰肿瘤细胞的增殖与分裂,抑制癌症生长.该药物主要用于研究卵巢癌、肺癌和乳腺癌等多种癌症.

Camptothecin-d5是Camptothecin的氘化衍生物.作为一种生物碱,Camptothecin (CPT) 具有抑制DNAtopoisomeraseI (Topo I) 的功能,其IC50值达到679 nM.此外,Camptothecin (CPT) 在结直肠癌、乳腺癌、肺癌和卵巢癌治疗中展现出显著的抗肿瘤效果,主要通过调节人类癌细胞中miRNA的表达模式来影响 hypoxia-inducible factor-1α (HIF-1α)的活性.

Exatecan Intermediate 5 作为Exatecan的中间体,其应用广泛.Exatecan (DX-8951),一个有效的DNA拓扑异构酶I (topoisomerase I) 抑制剂,具IC50为2.2 μM (0.975 μg/mL),主要用于癌症治疗研究.此外,Exatecan Intermediate 5 还关键于抗体-药物偶联物 (Antibody-Drug Conjugates (ADCs)) 的合成过程.

EGF Rligand-11，作为EGFR的特异性配体，主要用于PROTAC MS154的制备。

NMT-IN-7 是一种N-肉豆蔻酰转移酶 (NMT)抑制剂，其对HsNMT1M的IC50为2.1 nM，对SU-DHL-10细胞的毒性IC50为0.6 nM。NMT-IN-7 可用作ADC 细胞毒素。

Paclitaxel-d5(benzoyloxy) 为 Paclitaxel 的氘代物。Paclitaxel 是天然抗肿瘤药，能够稳定微管蛋白 (tubulin) 的聚合，导致有丝分裂停滞并诱发细胞凋亡 (apoptosis)，最终引起细胞死亡。此外，Paclitaxel 还能诱导细胞自噬 (autophagy)。