PDGFR

Famitinib malate is an orally active, multi-targeted kinase inhibitor primarily targeting c-kit, VEGFR-2, and PDGFRβ, with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively. This compound induces cell apoptosis and demonstrates significant anti-tumor activity in human gastric cancer cells and xenograft models. Famitinib malate is a valuable tool for research into cancer therapies and mechanisms of action.

Methylnissolin (Astrapterocarpan), a natural compound isolated from *Astragalus membranaceus*, inhibits PDGF-BB-induced vascular smooth muscle cell proliferation with an IC50 of 10 μM. It exerts its effects by suppressing PDGF-BB-induced phosphorylation of ERK1/2, thereby blocking activation of the ERK1/2 MAP kinase signaling cascade.

Tyrphostin AG1433 (SU1433) is a tyrosine kinase inhibitor that selectively targets platelet-derived growth factor receptor beta (PDGFRβ) and vascular endothelial growth factor receptor 2 (VEGFR-2/Flk-1/KDR), with IC₅₀ values of 5.0 μM and 9.3 μM, respectively. By inhibiting these key angiogenic receptors, AG1433 disrupts downstream signaling involved in endothelial cell proliferation and migration, thereby effectively preventing blood vessel formation (angiogenesis). It is a valuable compound for research into tumor angiogenesis, vascular disorders, and anti-angiogenic therapeutic strategies.

Chiauranib (CS2164) is an orally active, multi-targeted small molecule inhibitor with potent anticancer activity. It targets key kinases involved in tumor angiogenesis, including VEGFR1, VEGFR2, VEGFR3, PDGFRα, and c-Kit, as well as mitosis-related kinase Aurora B and inflammation-associated kinase CSF-1R. Chiauranib exhibits IC₅₀ values ranging from 1 to 9 nM against these targets. Through simultaneous inhibition of angiogenesis, cell division, and inflammation pathways, Chiauranib exerts strong antitumor effects and is a promising candidate for the treatment of various solid tumors.

Sennoside B is a potent inhibitor of platelet-derived growth factor receptor (PDGFR). It effectively suppresses cell proliferation and reduces the phosphorylation of PDGFR-β, STAT-5, AKT, and ERK in response to PDGF-BB stimulation. Additionally, Sennoside B exhibits gastroprotective properties and is suitable for research applications focused on gastritis and related gastrointestinal disorders.

GZD856 formic is a selective inhibitor of PDGFRα/β, displaying IC50 values of 68.6 nM and 136.6 nM, respectively, along with potent inhibition of Bcr-Abl, including the T315I mutant with IC50s of 19.9 nM and 15.4 nM. This compound exhibits notable antitumor activity, making it a valuable tool for cancer research. Additionally, GZD856 formic serves as a click chemistry reagent due to its alkyne group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, facilitating bioconjugation studies and compound labeling.

JI-101 hydrochloride is an orally active inhibitor targeting EphB4, VEGFR-2, and PDGFR-β, effectively modulating angiogenesis signaling pathways associated with tumor vasculature. This compound demonstrates significant anti-cancer activity, inhibiting multiple stages of tumor angiogenesis and showing efficacy against various cancer cell lines and xenografts. With rapid oral absorption and extensive tissue distribution, preferential uptake occurs in the lungs, while elimination primarily occurs via feces. JI-101 hydrochloride can be utilized in research studies focused on ovarian cancer and other solid tumors, providing valuable insights into angiogenesis and cancer treatment mechanisms.