pancreatic tumor

Pyrazoloacridine (PD 115934) is a nucleic acid binding agent that inhibits the activity of topo I and II with an IC50 of 1.25 μM in K562 cells. Pyrazoloacridine shows anti-cancer activity.

KU-2285 shows anti-tumor, anti-metastatic and anti-colony forming effects on mouse melanoma B16.KU-2285 can be used to study pancreatic cancer.

Akt3 degrader 1 is a specific Akt3 degrader with anticancer and antiproliferative activity that inhibits tumor growth in mice.Akt3 degrader 1 is used in the study of non-small cell lung cancer and pancreatic cancer.

AG-270 is an allosteric and orally active inhibitor of MAT2A.

JI130 is able to impair the ability of Hes1 to repress transcription. JI130 treatment significantly reduced tumor volume in a murine pancreatic tumor xenograft model.

Daunorubicin hydrochloride (Rubidomycin hydrochloride), an anthracycline aminoglycoside antineoplastic, inhibits DNA replication and repair and RNA and protein synthesis.

1. Berberine (Umbellatine) is a potent oral hypoglycemic agent with beneficial effects on lipid metabolism. 2. Berberine may as a broad-spectrum anti-microbial medicine, a complementary therapeutic agent for HIV/AIDS. 3. Berberine seems to act as an herbal antidepressant and a neuroprotector against neurodegenerative disorders. 4. Berberine is used in histology for staining heparin in mast cells. As a natural dye, berberine has a colour index of 7516. 5. Berberine reduces hepatic fat content in rats with nonalcoholic fatty liver disease; also prevents proliferation of hepatic stellate cells (HSCs), which are central for the development of fibrosis during liver injury. 6. Berberine can ameliorate proinflammatory cytokines-induced intestinal epithelial tight junction damage in vitro, and berberine may be one of the targeted therapeutic agents that can restore barrier function in intestinal disease states. 7. Berberine has antineoplastic effects, including breast cancer, leukemia, melanoma, epidermoid carcinoma, hepatoma, pancreatic cancer, oral carcinoma, tongue carcinoma, glioblastoma, prostate carcinoma and gastric carcinoma, etc.

ABzOH is a benzoic acid derivative, similar in structure to non-steroidal anti-inflammatory drugs such as aspirin, with anti-inflammatory, anti-tumor and anti-proliferative effects. ABzOH can not only inhibit the expression of tumor necrosis factor-α (TNF-a), interleukin-1β (IL-1β), interleukin-6 (IL-6) and other pro-inflammatory cytokines, but also inhibit breast cancer, lung cancer and pancreatic cancer.

p-Terphenyl is a triphenyl derivative used in industry as a heat transfer medium and dye carrier, and can be used for related research in the life sciences.

Cenisertib is A potent ATP-competitive multi-kinase inhibitor, showing inhibitory effects on the activity of Aurora-kinase-A B, ABL1, AKT, STAT5, FLT3, as well as kinase inhibitors of FER and its homolog. Cenisertib inhibits the growth of tumor mast cells (MCS) by inhibiting the activity of several different molecular targets. Cenisertib also inhibits tumor growth in pancreatic, breast, colon, ovarian and lung cancer and leukemia in xenograft models.

Sanggenon C is a flavanone Diels-Alder adduct compound isolated from the root bark of Morus alba. Sanggenon C can inhibit NF-κB activity, inhibit the expression of inducible nitric oxide synthase in RAW264.7 cells, and inhibit tumor necrosis factor-α-stimulated cell adhesion and vascular cell adhesion molecule-1 expression; Sanggenon C also has antioxidant and anti-inflammatory effects, and also has the effect of inhibiting pancreatic lipase. [1,2]

DHFR-IN-4 is a potent dihydrofolate reductase (DHFR) inhibitor with anti-tumor activity, which also inhibits EGFR and HER2, and is useful for studying pancreatic cancer.

AES-135 is a potent HDAC inhibitor, inhibits HDAC3, HDAC6, HDAC11 (IC50s: 654, 190, and 636 nM) with anti-tumor activity.

Nic-15 (compound 4n) serves as an anti-constrictive agent targeting the low vascular characteristics of pancreatic tumors. These characteristics enable cancer cells to adapt to the nutrient-deficient tumor microenvironment and develop resistance to treatment. Nic-15 modulates the PI3K Akt mTOR pathway and alleviates ER stress induced by Gemcitabine. It significantly inhibits migration and colony formation in MIA PaCa-2 and PANC-1 pancreatic cancer cells. When used in combination with Gemcitabine, Nic-15 effectively addresses resistance issues in pancreatic tumors. In xenograft models in vivo, Nic-15 notably enhances the efficacy of Gemcitabine.

WB436B, a highly selective STAT3 inhibitor, effectively targets and inhibits STAT3-Tyr705 phosphorylation along with the expression of STAT3 target genes. It exhibits cytotoxic effects on pancreatic cancer cells by inducing apoptosis. Furthermore, WB436B suppresses tumor growth and metastasis in pancreatic cancer mouse models, thereby prolonging the survival of tumor-bearing mice.

CAM2602 is an inhibitor of Aurora A-TPX2 interaction, demonstrating a binding affinity of 19 nM with Aurora A. This compound has been shown to inhibit the growth of pancreatic cancer cells. In solid tumor xenograft models, CAM2602 increases the proportion of PH3-positive cells while decreasing the ratio of P-Thr288Aurora A-positive cells, ultimately inhibiting tumor growth.

DSPE-PEG(2000) maleimide is a PEGylated derivative of 1,2-distearoyl-sn-glycero-3-phosphoethanolamine (DSPE). This compound is frequently utilized both in vitro and in vivo for synthesizing lipid nanoparticles (LNPs) that deliver siRNA or small molecule anticancer drugs. In experiments, LNPs containing DSPE-PEG(2000) maleimide and encapsulating siRNA targeting the mRNAs for p53 and K-RAS induced tumor regression in a PANC-1 pancreatic ductal adenocarcinoma mouse xenograft model.

68Ga-DOTA-NT-20.3 is an analogue of neurotensin (NTS) and acts as a ligand for 68Ga ions. In PET imaging, it demonstrates rapid tumor uptake and high contrast between tumor and background, along with fast clearance from the blood and moderate accumulation in the kidneys. Its pharmacokinetic and biodistribution properties are advantageous, producing high-quality PET images in mice with subcutaneous or orthotopic human pancreatic cancer xenografts. 68Ga-DOTA-NT-20.3 specifically binds to NTSR1 on pancreatic cancer cells and outperforms 18F-FDG in PET detection of adenocarcinoma.

Methylbenzoprim is an innovative multifunctional thymidylate synthase (TYMS) inhibitor. It exhibits greater antitumor activity compared to current fluoropyrimidines and antifolates, without inducing TYMS overexpression. In pancreatic xenograft tumor models and hTS Ink4a Arf null genetically engineered mouse models, Methylbenzoprim effectively prolongs survival.

SBI-183 is an orally active QSOX1 inhibitor (Kd: 20 μM). It can inhibit the proliferation and invasion phenotypes of renal carcinoma cell lines, triple-negative breast cancer cell lines, lung adenocarcinoma cell lines, and pancreatic ductal adenocarcinoma. In vivo, SBI-183 suppresses tumor growth in two human renal cell carcinoma xenograft mouse models.

Toyaburgine is an isoquinoline compound with anti-tumor activity. It disrupts the PI3K/AKT/mTOR signaling pathway, causing significant morphological changes and cancer cell death in MIA PaCa-2 cells, while also inhibiting cell migration and colony formation. Toyaburgine shows potential for use in pancreatic cancer research.

LNS8801 is an orally active agonist of the G protein-coupled estrogen receptor (GPER). By activating GPER, LNS8801 mediates downstream signaling pathways, such as promoting cAMP production and activating CREB signaling, which results in antitumor activities like inhibiting tumor cell proliferation, inducing cell differentiation, and enhancing tumor immunogenicity. It is applicable in research across various cancers, such as melanoma, pancreatic cancer, colorectal cancer, and lung cancer, as well as studies exploring the role of GPER in normal physiological and pathological processes.

Mogroside V is a widely used sweetener, has in vitro AMPK activating effect, it also has anti-inflammatory potential in murine macrophages and a murine ear edema model, and has the potential to protect against LPS-induced airway inflammation in a model of ALI. Mogroside V has antioxidant properties and possesses tumor growth inhibitory activity in pancreatic cancer models.

Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities, including antibacterial, anticancer, antiplatelet, and antioxidant properties.1,2,3,4It is active against Gram-positive (MICs = 5-160 µg/ml) and Gram-negative bacteria (MICs = 136-200 µg/ml), as well as yeasts (MICs = 10-20 µg/ml).1Ajoene is cytotoxic to mouse melanoma cells (IC50= 18 µM), as well as human colon, lung, mammary, and pancreatic cancer cells (IC50s = 7-41 µM).2It reduces tumor growth in a B16/BL6 mouse model of melanoma when administered at a dose of 25 mg/kg every other day and decreases the number of lung metastases when administered prior to tumor cell inoculation at doses ranging from 1-25 mg/kg. It inhibits ADP- or collagen-induced platelet aggregation in isolated baboon platelets when used at concentrations ranging from 75 to 150 µg/ml and in platelet-rich plasma isolated from baboons when administered at a dose of 25 mg/kg.3Ajoene (25 mg/kg) prevents thrombus formation on damaged arterial walls in heparinized pigs in anin situmodel of thrombogenesis.5It also reduces high-fat diet-induced hepatic steatosis, histopathological markers of liver damage, thiobarbituric acid reactive substances (TBARS) formation, and protein oxidation in a mouse model of non-alcoholic fatty liver disease (NAFLD).4 1.Naganawa, R., Iwata, N., Ishikawa, K., et al.Inhibition of microbial growth by ajoene, a sulfur-containing compound derived from garlicAppl. Environ. Microbiol.62(11)4238-4242(1996) 2.Taylor, P., Noriega, R., Farah, C., et al.Ajoene inhibits both primary tumor growth and metastasis of B16/BL6 melanoma cells in C57BL/6 miceCancer Lett.239(2)298-304(2006) 3.Teranishi, K., Apitz-Castro, R., Robson, S.C., et al.Inhibition of baboon platelet aggregation in vitro and in vivo by the garlic derivative, ajoeneXenotransplantation10(4)374-379(2003) 4.Han, C.Y., Ki, S.H., Kim, Y.W., et al.Ajoene, a stable garlic by-product, inhibits high fat diet-induced hepatic steatosis and oxidative injury through LKB1-dependent AMPK activationAntioxid. Redox Signal.14(2)187-202(2011) 5.Apitz-Castro, R., Badimon, J.J., and Badimon, L.A garlic derivative, ajoene, inhibits platelet deposition on severely damaged vessel wall in an in vivo porcine experimental modelThromb. Res.75(3)243-249(1994)