VEGFR Inhibitor

Gamabufotalin (Gamabufagin), a main active compound isolated from Chinese medicine Chansu, has been shown to strongly inhibit cancer cell growth and inflammatory response. Gamabufotalin could inhibite angiogenesis by inhibiting the activation of VEGFR-2 signaling pathways.

Dovitinib (lactate) (Standard) is the analytical standard of Dovitinib (lactate). This product is intended for research and analytical applications. Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively.

DW532 is a dual inhibitor of tubulin and tyrosine kinase, with IC₅₀ values of 4.9 μM and 5.5 μM against EGFR and VEGFR2, respectively, and a K_D of 3.6 μM for tubulin. DW532 induces cell cycle arrest at the G₂/M phase, triggers cell apoptosis via caspase-related pathways, and inhibits angiogenesis. DW532 can be used for research related to cancers (e.g., breast cancer).

Lenvatinib (mesylate) (Standard) is the analytical standard of Lenvatinib (mesylate). This product is intended for research and analytical applications. Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.

VEGFR-2-IN-44 (compound 4b) is a selective VEGF-R2 (Flk-1) inhibitor with an IC₅₀ value of 70 nM. VEGFR-2-IN-44 also inhibits PDGF-Rβ with an IC₅₀ of 920 nM.

Ningetinib (Standard) is the analytical standard of Ningetinib (HY-107145A). This product is intended for research and analytical applications. Ningetinib is a potent, orally bioavailable small molecule tyrosine K_inase inhibitor (TK_i) with IC₅₀s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.

19-epi-Scholaricine is an orally active indole alkaloid. 19-epi-Scholaricine downregulates the expression of profibrotic/apoptotic proteins (HRAS, HSP90AA1, KDR) and upregulates the expression of cell cycle-related protein (CDK2). 19-epi-Scholaricine suppresses ROS production and reduces the release of inflammatory mediators, thereby attenuating podocyte apoptosis, renal inflammation and oxidative stress by inhibiting AKT/mTOR. 19-epi-Scholaricine can be used in the research of chronic glomerulonephritis and membranous nephropathy.

Cremastranone is an antiangiogenic homoisoflavone. Cremastranone can inhibit HUVECs cell proliferation, with a GI₅₀ value of 1.5 uM.

Semaxinib (Standard) is the analytical standard of Semaxinib (HY-10374). This product is intended for research and analytical applications. Semaxinib (SU5416) is a potent and selective inhibitor of VEGFR (Flk-1/KDR) with an IC₅₀ of 1.23 μM.

VEGFR-2-IN-87 is a VEGFR-2 inhibitor with an inhibition rate of 79% in enzymatic assays. VEGFR-2-IN-87 exhibits anti-angiogenic activity. VEGFR-2-IN-87 can be used in cancer research.

1,3,5-Tricaffeoylquinic acid acts as an angiogenesis inhibitor and apoptosis inducer, and exhibits anti-HIV activity. 1,3,5-Tricaffeoylquinic acid inhibits the phosphorylation of VEGFR2, ERK, PI3K, Akt and mTOR in the angiogenesis signaling pathway. 1,3,5-Tricaffeoylquinic acid regulates apoptosis-related proteins, upregulates the levels of activated caspase-8, Bax, activated PARP and caspase-3/9, while downregulates the level of Bcl-2. 1,3,5-Tricaffeoylquinic acid inhibits tube formation and shows cytotoxicity against ovarian cancer cells. 1,3,5-Tricaffeoylquinic acid can be used in studies related to ovarian cancer.

Isomangiferin (Standard) is the analytical standard of Isomangiferin (HY-N0772). This product is intended for research and analytical applications. Isomangiferin is an orally active xanthone C-glucoside, and its chemical structure is similar to Mangiferin (HY-N0290). Isomangiferin is an effective VEGFR-2 kinase inhibitor, which can induces cell apoptosis, inhibit the growth, metastasis and angiogenesis of breast cancer. Isomangiferin exerts anti-inflammatory effects by inhibiting the HMGB1/NLRP3/NF-κB signaling pathway, thereby improving the renal function indicators of diabetic mice. Isomangiferin exhibits inhibitory effects on various bacteria and herpes simplex virus type 1 (HSV-1). Isomangiferin promotes the migration and osteogenic differentiation of bone marrow mesenchymal stem cells (BMSCs) and reduces cell apoptosis and the production of ROS by activating the AMPK/ACC pathway, thereby facilitating fracture healing.

YLL545 is a type of vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor. YLL545 can inhibit VEGF-induced phosphorylation of VEGFR2 and the activation of downstream signaling factors (like phosphorylated STAT3 and phosphorylated ERK1/2) in human umbilical vein endothelial cells (HUVEC). YLL545 can suppress the proliferation, migration, invasion, and angiogenesis of HUVEC. YLL545 can induce apoptosis in breast cancer mice and inhibit tumor growth.

Pazopanib-d₃ (hydrochloride) (GW786034-d₃ (hydrochloride)) is deuterium labeled Pazopanib (Hydrochloride). Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC₅₀ of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.

Vorolanib (Standard) is the analytical standard of Vorolanib (HY-109019). This product is intended for research and analytical applications. Vorolanib (CM082) is an orally active, potent multiK_inase VEGFR/PDGFR inhibitor. Vorolanib is a potent ATP-binding cassette (ABC) transporter inhibitor. Vorolanib is an angiogenesis inhibitor and has antitumor activity combined with ZD1839 (HY-50895).

RAF265 (Standard) is the analytical standard of RAF265 (HY-10248). This product is intended for research and analytical applications. RAF265 is a potent and orally active RAF/VEGFR2 inhibitor.

VEGFR-IN-6 (Compound 3) is a vascular endothelial growth factor receptor (VEGFR) inhibitor. VEGFR-IN-6 can inhibit angiogenesis. VEGFR-IN-6 is promising for research of tumor diseases that rely on angiogenesis.

ENMD-2076 (Standard) is the analytical standard of ENMD-2076 (HY-10987A). This product is intended for research and analytical applications. ENMD-2076 is a multi-targeted K_inase inhibitor with IC₅₀s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, K_dR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.

SYHA1815 is an orally active RET inhibitor (IC₅₀=0.9 nmol/L) with antitumor activity. SYHA1815 is more selective for RET than KDR (IC₅₀=15.9 nmol/L). SYHA1815 arrests the G1 cell cycle and inhibits RET-driven cell proliferation by downregulating c-Myc.

(Z)-FeCP-oxindole (Standard) is the analytical standard of (Z)-FeCP-oxindole (HY-108444). This product is intended for research and analytical applications. (Z)-FeCP-oxindole is a selective human vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with an IC₅₀ value of 200 nM. (Z)-FeCP-oxindole can significantly inhibit VEGFR1 and PDGFRa or b at 10 μM. (Z)-FeCP-oxindole has some anticancer activity, acting on B16 murine melanoma lines with IC₅₀ less than 1 μM.