dna-crosslinking

6-Aminonicotinamide 是一种竞争性 NADP+依赖性酶，是一种烟酰胺抗代谢药，葡萄糖 6-磷酸脱氢酶抑制剂 (Ki=0.46 μM)。 它干扰糖酵解，导致 ATP 耗竭，并与 DNA 交联化学疗法药物，如Cisplatin，协同杀死癌细胞。

MC-Val-Ala-PBD is a drug-linker conjugate for ADC by using the antitumor antibiotic, pyrrolobenzodiazepine (PBD, a cytotoxic DNA crosslinking), linked via the cleavable linker MC-Val-Ala[1].

Amotosalen hydrochloride (S-59) is a light-activated, RNA-, DNA-crosslinking psoralen compound and is used to neutralize pathogens.

Metamelfalan is an alkylating nitrogen mustard with potential antineoplastic activity. It causes crosslinking of DNA, thereby preventing DNA replication and eventually cellular proliferation.

Ametantrone Acetate is a topoisomerase II inhibitor of anthrapyrazole family, which can lead to DNA covalent crosslinking.

cDPCP is a platinum-containing DNA-crosslinking agent.1Unlike cisplatin or oxaliplatin , cDPCP forms monofunctional DNA adducts. It is transported into cells by organic cation transporter 1 (OCT1) and OCT2, inhibiting proliferation of MDCK cells expressing the human transporters with IC50values of 8.1 and 1.5 μM, respectively. cDPCP inhibits RNA polymerase II-mediated transcription in a reporter assay using HeLa cells. It increases survival in murine S180 sarcoma and P388 leukemia models when administered at doses of 40 and 80 mg/kg, respectively.2 1.Lovejoy, K.S., Todd, R.C., Zhang, S., et al.cis-Diammine(pyridine)chloroplatinum(II), a monofunctional platinum(II) antitumor agent: Uptake, structure, function, and prospectsProc. Natl. Acad. Sci. USA105(26)8902-9807(2008) 2.Hollis, L.S., Amundsen, A.R., and Stern, E.W.Chemical and biological properties of a new series of cis-diammineplatinum(II) antitumor agents containing three nitrogen donors: cis-[Pt(NH3)2(N-donor)Cl]+J. Med. Chem.32128-136(1989)

EC2629 is a highly potent folate- receptor-targeted DNA crosslinking agent.

Bisantrene (CL216942) 是一种具有抗肿瘤活性的蒽基双腙，可靶向作用于真核生物的 II 型拓扑异构酶。它插入并破坏 DNA 的构型，导致 DNA 单链断裂、DNA-蛋白质交联和 DNA 复制的抑制。

(rel)-Oxaliplatin is a DNA synthesis inhibitor that induces DNA crosslinking damage, inhibits DNA replication and transcription, and stimulates apoptosis. This compound has applications in cancer research [1] [2] [3].

Oxaliplatin-d10 is intended for use as an internal standard for the quantification of oxaliplatin by GC- or LC-MS. Oxaliplatin is a platinum-containing DNA-crosslinking agent. It induces the formation of DNA inter- and intrastrand crosslinks and DNA-protein adducts, inhibits DNA and RNA synthesis, and induces apoptosis in cancer cells. Oxaliplatin is cytotoxic to cisplatin-sensitive A2780(1A9) and KB-3-1 cells and cisplatin-resistant A2780-E(80) and KB-CP20 cells (IC50s = 0.12, 0.39, 4.7, and 2.7 µM, respectively). It reduces tumor growth in an HCCLM3 mouse xenograft model when administered at doses of 5 or 10 mg kg once per week. Formulations containing oxaliplatin have been used in the treatment of advanced colorectal cancer and as adjuvants in stage III colon cancer.

Busulfan-d8 (Sulphabutin-d8)  是 2H 标记的 Busulfan。Busulfan 是一种有效的烷化抗肿瘤剂，是一种免疫抑制和清髓性化疗活性分子，具有细胞和抗肿瘤活性，通过交联 DNA 以及 DNA 和蛋白质造成 DNA 损伤。