oxaliplatin

Oxaliplatin (L-OHP) is a DNA alkylating agent, an inhibitor of DNA synthesis. Oxaliplatin causes DNA cross-linking damage, preventing DNA replication and transcription and leading to cell death. Oxaliplatin induces autophagy.

(rel)-Oxaliplatin, a DNA synthesis inhibitor, 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.

1. Cinnamaldehyde (Cinnamic Aldehyde) has antipyretic activity. 2. Cinnamaldehyde is a sedative agent. 3. Cinnamaldehyde inhibits invasive capabilities of MDA-MB-435S cells was correlated with down-regulating the expression of miR-27a. 4. Cinnamaldehyde induces the generation of reactive oxygen species and exerts vasodilator and anticancer effects. 5. Cinnamaldehyde appears to be a promising candidate as an adjuvant in combination therapy with 5-fluorouracil (5-FU) and oxaliplatin (OXA), two chemotherapeutic agents used in CRC treatment. The possible mechanisms of its action may involve the regulation of drugmetabolizing genes. 6. Cinnamaldehyde plays a certain role in inhibiting the occurrence and progression of melanoma and its action mechanism may be manifested by inhibiting expression of VEGF and HIF-α, thus blood vessel simulation and formation of new blood vessels of melanoma cells, and growth of tumors accordingly.

DL-Syringaresinol ( (±)-Syringaresinol) is a lignan from ginseng berries with anti-inflammatory, antioxidant, analgesic and weak anti-mycobacterial activities.DL-Syringaresinol can delay oxidative stress-induced skin aging through autophagy, alleviate oxaliplatin-induced neuropathic pain and sepsis-induced cardiac dysfunction by inhibiting inflammatory responses. neuropathic pain and sepsis-induced cardiac dysfunction by inhibiting inflammatory responses.

Copper histidine inhibited Ctr1-mediated cellular uptake of oxaliplatin in vitro without altering oxaliplatin accumulation of platinum or neurotoxicity in DRG tissues in vivo. Copper histidine is administered orally for the treatment of Menkes disease.

Ethaselen (BBSKE) is an orally active and selective thioredoxin reductase 1 (TrxR) inhibitor with anticancer activity that directly inhibits TrxR1 activity and is commonly used in combination with oxaliplatin to inhibit tumor growth.Ethaselen induces apoptosis in cancer cells and inhibits the proliferation of colorectal cancer cells.

Osemitamab, an IgG1 antibody, targets human claudin-18.2 and comprises a human-Mus musculus monoclonal TST001 γ1-chain disulfide-bonded to a human-Mus musculus monoclonal TST001 κ-chain dimer (ACI). It is utilized, in conjunction with Capecitabine and Oxaliplatin, for gastric/gastroesophageal junction (G/GEJ) cancer studies [1] [2].

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

4-(3,4-Difluorobenzo)curcumin (CDF) is a semisynthetic coumarin noted for its antiparasitic and anticancer properties. It effectively reduces the population of Vero cells infected by T. gondii promastigotes and amastigotes, with EC50 values of 0.8 and 0.37 µM, respectively. Furthermore, at concentrations of 4 and 8 µM, CDF enhances the efficacy of 5-fluorouracil and oxaliplatin in inhibiting the formation of both primary and secondary colonospheres in chemoresistant HCT116 cells.

TREM2-IN-1 (OPA), an inhibitor derived from oxaliplatin and artesunate, alleviates the immunosuppressive tumor microenvironment and enhances the efficacy of chemical anticancer treatments [1].

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

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)

Neoline is an active ingredient of A. venetum root (PA) that ameliorates oxaliplatin-induced peripheral neuropathy in mice.Neoline inhibits Nav1.7 voltage-gated sodium channel currents (VGSC). It can be used as a labeling compound to determine the quality of PA products used in the study of neuropathic pain.