antitumor properties

AAL-993 is a potent VEGFR inhibitor with IC50s of 130 nM, 23 nM and 18 nM for VEGFR1, VEGFR2 and VEGFR3, respectively. AAL993 has a weak inhibitory effect on other tyrosine kinases. AAL993 also shows potent antiangiogenic and antitumor activities.

Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6/22/90/15/20/20/57/58 nM) with oral activity. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.

Doxycycline (hyclate) is an orally active tetracycline antibiotic with broad-spectrum inhibitory activity against matrix metalloproteinases (MMPs), possessing both antibacterial and antitumor properties, and is commonly used in inducible gene expression ON-OFF systems.

Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.

Chloroquinoxaline sulfonamide (Chloroquinoxaline) is a topoisomerase II alpha/beta toxin with antitumor activity and immunosuppressive properties that inhibits the proliferation of B16 melanoma cells in mice, and can be used to study metastatic colorectal cancer. It can be used to study metastatic colorectal cancer.

A-176120 ammonium is a novel farnesyl pyrophosphate analog with antitumor and antiangiogenic properties and inhibits farnesyltransferase activity.

BPDA2 is a highly selective and competitive SHP2 inhibitor, exhibiting IC50 values of 92.0 nM for SHP2, and 33.39 μM and 40.71 μM for SHP1 and SHP1B, respectively. This compound effectively downregulates mitogenic and cell survival signaling, including reducing expression of receptor tyrosine kinases (RTKs). Furthermore, BPDA2 suppresses SHP2-mediated signaling, leading to the inhibition of breast cancer cell phenotypes [1].

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].

Cyanoacetohydrazide (Cyanoacetic hydrazide) is an anti-TB drug. It has also been used to derive compounds that may have antitumor properties.

Genistein (NPI 031L) is a naturally occurring soy isoflavone, a multi-targeted tyrosine kinase inhibitor. Genistein has antitumor, antioxidant, and anthelmintic properties, and also produces estrogen-like effects in the body.

Notoginsenoside R1 (Sanchinoside R1) has been shown to exhibit antioxidant, antiapoptotic, anti-inflammatory, and immune-stimulatory properties.

Squalene (AddaVax) is an intermediate in cholesterol synthesis. Squalene has a variety of pharmacological properties, such as antilipemic, hepatoprotective, anti-atherosclerotic, cardioprotective, antioxidant, antitumor and antifungal.

Tetraethylammonium chloride is a quaternary ammonium compound. It is a non-selective potassium channel blocker. It is a good substrate for organic cation transporter proteins and has antitumor properties.

2-(2-fluoro-6-methoxyphenyl)pyrimidine-4-carboxylic acid is commonly used to synthesize compounds with anticancer and antitumor properties.

SphK1&2-IN-1, a sphingosine kinase inhibitor, exhibits anti-inflammatory, antitumor, and hemostatic properties.

Fulvene-5 is a chemical compound that exhibits antitumor activity. It functions as a potent inhibitor of NADPH oxidase 4 (NOX4) and possesses antioxidant properties. Additionally, Fulvene-5 acts as a reactive oxygen species (ROS) modifying agent and a powerful radioprotector.

Azadirachtin B (Deacetylazadirachtinol) is a terpenoid compound isolated from Azadirachta seeds, with insecticidal, anticancer, anti-inflammatory, antitumor, and antiviral activities, useful in the study of viral infections. Azadirachtin B also has osteoblast proliferation, differentiation, and mineralization properties.

Berberine chloride hydrate (Natural Yellow 18 chloride hydrate) is an alkaloid with antibiotic properties, antitumor activity, and the ability to induce reactive oxygen species (ROS) generation and inhibit DNA topoisomerase.

MC-Val-Cit-PAB-clindamycin is an antibody-drug conjugate (ADC) linker combining the potent antitumor properties of clindamycin, a protein synthesis inhibitor, with the ADC linker MC-Val-Cit-PAB, thereby enhancing its cancer cell targeting and killing effectiveness.

MC-Val-Cit-PAB-MMAF is an antibody-drug conjugate (ADC) component that exhibits antitumor properties through the action of the tubulin inhibitor, monomethyl auristatin F (MMAF), which is connected by a cathepsin-cleavable linker, MC-Val-Cit-PAB.

Antitumor photosensitizer-7 (compound 15), a photosensitizer possessing anti-cancer properties, demonstrates substantial cytotoxic effects on the G361 melanoma cell line when exposed to 414 nm blue light irradiation.

N-ω-chloroacetyl-L-ornithine (NCAO) serves as a powerful reversible competitive inhibitor of ornithine decarboxylase (ODC), displaying cytotoxic and antiproliferative properties against various tumor cell lines, with EC50 values spanning from 1 to 50.6 µM. In vitro studies reveal that NCAO promotes Apoptosis and restricts tumor cell migration. Additionally, it demonstrates significant antitumor efficacy in a mouse model, targeting both solid and ascitic tumors using the myeloma (Ag8) cell line. NCAO holds promise in the development of antitumor agents.

3-Demethylthiocolchicine, a colchicine analog, exhibits broad-spectrum antitumor activity and shares similar properties and activities with colchicine in inhibiting casein-induced amyloidosis, microtubule binding, and anti-inflammatory effects. Notably, it has significantly lower toxicity compared to colchicine.

Antitumor agent-188 (compound C6) exhibits α-glucosidase inhibitory activity and anticancer properties. It induces excessive ROS production, thereby triggering oxidative stress.