gastric cancer

HLY78 (4-Ethyl-5-methyl-5,6-dihydro-[1,3]dioxolo[4,5-j]phenanthridine) targets the DIX domain of Axin, is an activator of the Wnt/β-catenin signaling pathway and can enhance Axin-LRP6 binding to promote Wnt signaling.

Ibuprofen (Advil) is a propionic acid derivate and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic effects. Ibuprofen inhibits the activity of cyclo-oxygenase I and II, resulting in a decreased formation of precursors of prostaglandins and thromboxanes.

Rebamipide (OPC12759) is a quinolinone derivative with anti-ulcer and anti-inflammatory activities. Rebamipide induces cyclooxygenase 2 (COX2) synthesis which results in an increase in endogenous prostaglandin synthesis in the gastric mucosa. This agent also inhibits H. pylori-induced production of tumor necrosis factor (TNF) alpha and subsequent inflammation of the gastric mucosa. In addition, rebamipide scavenges oxygen-derived free radicals that potentially cause mucosal injury, and stimulates prostaglandin EP4 receptor gene expression followed by mucous secretion, thereby enhancing the gastric mucosal defense.

Levobupivacaine is an amino-amide local anaesthetic drug belonging to the family of n-alkylsubstituted pipecoloxylidide. It is the S-enantiomer of bupivacaine. Levobupivacaine hydrochloride is commonly marketed by AstraZeneca under the trade name Chirocaine. Compared to bupivacaine, levobupivacaine is associated with less vasodilation and has a longer duration of action. It is approximately 13 per cent less potent (by molarity) than racemic bupivacaine.Levobupivacaine is indicated for local anaesthesia including infiltration, nerve block, ophthalmic, epidural and intrathecal anaesthesia in adults; and infiltration analgesia in children. Adverse drug reactions (ADRs) are rare when it is administered correctly. Most ADRs relate to administration technique (resulting in systemic exposure) or pharmacological effects of anesthesia, however allergic reactions can rarely occur.

Neratinib (HKI-272) (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor for HER2 and EGFR (IC50: 59/92 nM), respectively.

Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a reversible neuronal sodium channel inhibitor and the pure S(-)-enantiomer of bupivacaine, used as a long-acting local anesthetic.

(E/Z)-BCI (NSC-150117), a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory properties, reduces LPS-induced inflammatory mediators and ROS production in macrophage cells by activating the Nrf2 signaling axis and inhibiting the NF-κB pathway.

CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.

Ibuprofen Lysine (Neoprofen) is a non-steroidal anti-inflammatory drug.

Ramucirumab, a human VEGFR-2 antagonist, is used for the treatment of solid tumors.

EIPA (L593754) is a TRPP3 channel inhibitor (IC50=10.5 μM) and an inhibitor of Na+/H+ exchange (NHE). EIPA inhibits megacytosis, promotes autophagy, and can be used in inflammation and tumor studies.

Trastuzumab deruxtecan (T-DXd) is an antibody-drug conjugate functioning as a HER2-targeted topoisomerase I inhibitor, with targeting capability and antitumor activity, employed in research on HER2-positive breast cancer and gastric cancer.

Disitamab vedotin (RC48) is an antibody-drug conjugate (ADC) and a HER2-targeted cytotoxic agent, consisting of an anti-HER2 monoclonal antibody conjugated to MMAE via a cleavable linker, used for the treatment of HER2-expressing solid tumors including gastric cancer, breast cancer, and urothelial carcinoma.

Trastuzumab is a humanized monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab has been clinically used to treat HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer.

Semaglutide is a long-acting, selective, competitive GLP-1R agonist and a long-acting analog of human glucagon-like peptide-1, exhibiting potent hypoglycemic, weight-loss, cardioprotective, and neuroprotective effects. Upon activation of the GLP-1R, semaglutide promotes insulin secretion, inhibits gastric emptying and appetite, while also enhancing autophagy and suppressing oxidative stress and apoptosis. Semaglutide also plays a role in regulating mitochondrial function and lipid metabolism. Semaglutide is being investigated for use in type 2 diabetes, obesity, Parkinson’s disease, metabolic and fatty liver diseases (MASLD), and other neurodegenerative and liver diseases, as well as in cancer research.

HRO761 (Werner syndrome RecQ helicase-IN-1, Example 42) is a small molecule inhibitor, a potent WRN inhibitor with high efficacy, and can be used for research on cancers such as colon cancer and gastric cancer.

Cadonilimab (AK104) is a tetravalent PD-1/CTLA-4 bispecific humanised antibody that activates T cells by enhancing IL-2 and IFN-γ secretion while reducing pro-inflammatory cytokine secretion (e.g., IL-6, IL-8). It offers low toxicity and high affinity, making it suitable for metastatic cervical, gastric, hepatic, and pulmonary cancers, pancreatic cancer, and oesophageal squamous cell carcinoma.

R1498 is an inhibitor of cyclin-dependent kinase 2. It also acts by targeting angiogenesis and mitosis pathways. It is well-tolerated and orally active for hepatocellular carcinoma and gastric cancer treatment.

Emitefur (BOF-A 2) is an orally active and potent 5-fluorouracil derivative with anticancer and antitumor activity.Emitefur is used in advanced gastric cancer, breast cancer and metabolism-related diseases.

K00135 (IMIDAZOPYRIDAZIN 1) is a selective inhibitor of Pim kinases and can be used in studies about gastric cancer and antileukemic therapeutics.

Topixantrone 2HCl is a DNA topoisomerase inhibitor with antitumor activity for the study of gastric and prostate cancer.

Famitinib (SHR1020) is a potent orally active multi-targeted kinase inhibitor that effectively inhibits the activity of c-kit, VEGFR-2, and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively [1]. It demonstrates remarkable antitumor properties in human gastric cancer cells and xenografts, inducing apoptosis [2].

Indomethacin is an orally active nonsteroidal anti-inflammatory drug (NSAID) that non-selectively inhibits cyclooxygenase enzymes COX-1 and COX-2, with IC₅₀ values of 18 nM and 26 nM, respectively. It exhibits good blood-brain barrier permeability and shows significant anti-inflammatory, anti-tumor, and anti-infective activities. Indomethacin is widely used in research related to cancer, inflammation, and viral infections, and is also commonly used to induce gastric ulcer models in animals.

N-Nitroso-N-methylurea (NMU/MNU/NMH) is a nitrosourea compound with alkylating, carcinogenic, and mutagenic properties; as a direct-acting alkylating agent, it interacts with DNA and targets multiple animal organs to induce various cancers and degenerative diseases, and is commonly used to induce disease models such as gastric cancer and breast cancer in mice.