VEGFR Inhibitor

Ripretinib (Standard) is the analytical standard of Ripretinib. This product is intended for research and analytical applications. Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2). DCC-2618 exerts antineoplastic effect and induces apoptosis.

Brivanib (alaninate) (Standard) is the analytical standard of Brivanib (alaninate). This product is intended for research and analytical applications. Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ.

ZM-306416 (CB-676475) hydrochloride is a potent VEGFR inhibitor with IC₅₀s of 0.1 μM and 2 μM for KDR and Flt, respectively. ZM-306416 hydrochloride is also a EGFR inhibitor with an IC₅₀ of <10 nM.

Tivozanib (hydrochloride hydrate) (Standard) is the analytical standard of Tivozanib (hydrochloride hydrate). This product is intended for research and analytical applications. Tivozanib hydrochloride hydrate is the hydrate hydrochloride form of Tivozanib (HY-10977). Tivozanib hydrochloride hydrate is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib hydrochloride hydrate exhibits antitumor efficacy.

Monosialoganglioside GM3 (bovine) is a monosialoganglioside and an inhibitor of VEGFR2 and Akt. At a concentration of 20 μM, Monosialoganglioside GM3 inhibits angiogenesis and reduces the proliferation and migration of human umbilical vein endothelial cells (HUVECs) by inhibiting VEGFR2 and Akt phosphorylation. Ganglioside GM3 also inhibits ferroptosis, providing protective effects during the formation of abdominal aortic aneurysms. Additionally, Monosialoganglioside GM3 (bovine) acts as an inhibitor of insulin signaling, inducing the dissociation of the insulin receptor (IR)-Caveolin-1 complex from lipid microdomains and causing insulin resistance in adipocytes. Monosialoganglioside GM3 (bovine) can be used in cancer and metabolic disease research.

Regorafenib (Hydrochloride) (Standard) is the analytical standard of Regorafenib (Hydrochloride). This product is intended for research and analytical applications. Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.

AFG210 is a potent multi-target kinase inhibitor that primarily inhibits Abl kinase (IC₅₀=330 nM), and also has inhibitory effects on other kinases such as B-Raf, C-Raf, FGFR-1, RET and VEGF receptors. AFG210 can be used to study chronic myeloid leukemia and other diseases with abnormal activation of Abl kinase.

Ponatinib (Standard) is the analytical standard of Ponatinib. This product is intended for research and analytical applications. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC₅₀s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.

Ponatinib (hydrochloride) (Standard) is the analytical standard of Ponatinib (hydrochloride). This product is intended for research and analytical applications. Ponatinib hydrochloride (AP24534 hydrochloride) is a hydrochloride of ponatinib. Ponatinib is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.

K00546 (Standard) is the analytical standard of K00546 (HY-103647). This product is intended for research and analytical applications. K00546 is a potent CDK1 and CDK2 inhibitor with IC₅₀s of 0.6 nM and 0.5 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. K00546 is also a potent CDC2-like kinase 1 (CLK1) and CLK3 inhibitor with IC₅₀s of 8.9 nM and 29.2 nM, respectively.

Cediranib (Standard) is the analytical standard of Cediranib. This product is intended for research and analytical applications. Cediranib (AZD2171) is a highly potent, orally available VEGFR tyrosine kinase inhibitor with IC₅₀s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.

Telatinib (mesylate) (Standard) is the analytical standard of Telatinib (mesylate). This product is intended for research and analytical applications. Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2, VEGFR3, PDGFα, and c-Kit inhibitor with IC50s of 6 nM, 4 nM, 15 nM and 1 nM, respectively.

ZK-261991 is an orally active VEGFR tyrosine kinase inhibitor with an IC₅₀ of 5 nM for VEGFR2.

BMS-690514 (Standard) is the analytical standard of BMS-690514 (HY-10333). This product is intended for research and analytical applications. BMS-690514 is a potent and orally active inhibitor of EGFR and VEGFR; has IC₅₀s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively.

JK-P3 (Standard) is the analytical standard of JK-P3 (HY-108933). This product is intended for research and analytical applications. JK-P3 is a potent and pan VEGFR2 inhibitor, with IC₅₀s of 7.83 μM, 27 μM and 5.18 μM for VEGFR2, FGFR1 and FGFR3, respectively. JK-P3 can inhibit VEGF-A-stimulated VEGFR2 activation and intracellular signalling, also inhibits endothelial monolayer wound closure and angiogenesis, as well as fibroblast growth factor receptor K_inase activity in vitro. JK-P3 has anti-angiogenic activity.

ENMD-2076 Tartrate (Standard) is the analytical standard of ENMD-2076 (Tartrate) (HY-10987). This product is intended for research and analytical applications. ENMD-2076 Tartrate 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.

Vandetanib trifluoroacetate (D6474 trifluoroacetate) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC₅₀=40 nM). Vandetanib trifluoroacetate also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC₅₀=110 nM) and EGFR/HER1 (IC₅₀=500 nM).

Naphazoline (Standard) is the analytical standard of Naphazoline (HY-111326). This product is intended for research and analytical applications. Naphazoline (Naphthazoline) is a potent α-adrenergic receptor agonist. Naphazoline reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytoK_ines (IFN-γ and IL-4), IgE, GMCSF, and NGF. Naphazoline can be used for non-bacterial conjunctivitis research.

Pazopanib (Standard) is the analytical standard of Pazopanib. This product is intended for research and analytical applications. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC₅₀s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.

VEGFR2-IN-4 (compound 25) is a potent and selective VEGFR2 kinase inhibitor, with a GI₅₀ of 0.7 nM. VEGFR2-IN-4 shows anti-angiogenic effect. VEGFR2-IN-4 can be used for the research of rheumatoid arthritis.