oxaliplatin

Oxaliplatin (L-OHP) 是一种 DNA 烷化剂，一种 DNA 合成抑制剂。Oxaliplatin 会导致 DNA 交联损伤，阻止 DNA 复制和转录并导致细胞死亡。Oxaliplatin 可以诱导细胞自噬。

(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.

ML-077, also known as VU0255011, is a highly selective, potent, saline soluble, best in class KCC2 antagonist for high fidelity in vitro studies on KCC2 function with IC(50)=537 nM. ML-077 is cell permeable and exhibits submicromolar potency

Neoline 是一种乌头根 (PA) 的活性成分，可改善奥沙利铂引起的小鼠周围神经病变。Neoline 通对Nav1.7 电压门控钠通道电流 (VGSC)有抑制作用。它可用作标记化合物，从而测定用于研究神经性疼痛的 PA 产品的质量。

Ethaselen (BBSKE) 是具有口服活性和选择性的硫氧还蛋白还原酶1 (TrxR) 抑制剂，具有抗癌活性，直接抑制 TrxR1 活性，常用奥沙利铂联合使用来抑制肿瘤生长。Ethaselen 可诱导癌细胞凋亡，抑制结直肠癌细胞增殖。

Copper histidine 抑制了Ctr1介导的奥沙利铂在体外的细胞摄取，而不会改变奥沙利铂在体内DRG 组织中的铂或神经毒性的积累。Copper histidine 通过口服治疗 Menkes 疾病。

Cinnamaldehyde (Cinnamic Aldehyde) 具有解热作用。 它是镇静剂。它抑制MDA-MB-435S 细胞的侵袭能力与下调miR-27a 的表达有关。它诱导活性氧的产生，发挥血管扩张和抗癌作用。 它似乎是一种有希望的候选药物，可作为与 5-氟尿嘧啶 (5-FU) 和奥沙利铂 (OXA) 这两种用于 CRC 治疗的化疗药物联合治疗的辅助剂。其作用的可能机制可能涉及药物代谢基因的调节。 它在抑制黑色素瘤的发生和发展方面具有一定的作用，其作用机制可能表现为抑制VEGF 和HIF-α的表达，从而使血管模拟和黑色素瘤细胞新生血管的形成，促进肿瘤的生长。

Ch282-5是一种口服的Bcl-2抑制剂，作用机制包括破坏线粒体自噬及mTOR通路，从而诱导依赖线粒体的细胞凋亡(Apoptosis)。该化合物不仅在体外实验中展现出对结肠癌细胞的抗增殖效果，而且在体内也能有效抑制其转移。此外，Ch282-5通过降低Mcl-1蛋白的表达和增加血小板数量，增强了Oxaliplatin引起的细胞自噬效应(Autophagy)，同时也有助于缓解Navitoclax的不良反应。

ADS1017 是一种组胺受体 (histamine receptor) 和毒蕈碱受体 (muscarinic receptor) 的拮抗剂，展现出对 hH3R、hH4R、hM2R 和 hM4R 的良好亲和力，pKi 值分别为 6.8、5.5、7.4 和 7.2。在Capsaicin或Oxaliplatin诱导的小鼠疼痛模型中，ADS1017 展示出显著的镇痛和抗痛觉过敏的效果。

Phenanthriplatin, also known as cis-[Pt(NH3)2-(phenanthridine)Cl]NO3, is a new drug candidate. It belongs to a family of platinum(II)-based agents which includes cisplatin, oxaliplatin and carboplatin. Phenanthriplatin Acts As a Covalent Poison of Topoiso

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)

Osemitamab是一种针对人类claudin-18.2的IgG1单克隆抗体。它由来自人鼠嵌合体TST001的γ-1链与κ链通过二硫键连接而成的二聚体(ACI)构成。该化合物与Capecitabine和Oxaliplatin联合应用，适用于胃(G)及胃食管结合部(GEJ)癌症的研究。

4-(3,4-Difluorobenzo)curcumin（CDF）是一种具有抗寄生虫和抗癌活性的半合成香豆素。它能减少被T. gondii持鞭毛体和无鞭毛体感染的Vero细胞的数量（EC50s分别为0.8和0.37 µM）。CDF（4和8 µM）通过增强5-氟尿嘧啶和奥沙利铂对化药抵抗性HCT116细胞主要和次要结肠球形成的抑制作用。

DL-Syringaresinol ( (±)-Syringaresinol) 是一种来自与人参浆果的木质素，具有抗炎、抗氧化、镇痛活性和较弱的抗分枝杆菌活性。DL-Syringaresinol 可通过自噬延缓氧化应激诱导的皮肤老化，通过抑制炎症反应来缓解奥沙利铂诱导的神经性疼痛和脓毒症引起的心功能障碍。