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Catalog No.
Product Name
Application
Product Information
Citations
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VEGFR-2/FGFR inhibitor
CP-547632 hydrochloride is a well-tolerated, orally-bioavailable inhibitor of the VEGFR-2 and basic fibroblast growth factor (FGF) kinases with IC50s of 11 nM and 9 nM, respectively. -
VEGFR-2 inhibitor
JNJ-38158471 is a well tolerated, orally available, highly selective VEGFR-2 inhibitor, with an IC50 of 40 nM. JNJ-38158471 also inhibits Ret and Kit with IC50s of 180 and 500 nM, respectively. -
VEGFR2 inhibitor
ZM323881 hydrochloride is a potent and selective VEGFR2 inhibitor with an IC50 of less than 2 nM. -
VEGFR2 inhibitor
VEGFR-2-IN-5 is a VEGFR2 inhibitor extracted from patent WO2013055780A1, Page 31. -
ATP-competitive multitargeted kinase inhibitor
Ilorasertib (ABT-348) is a potent and ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A with IC50s of 1 nM, 7 nM, 120 nM, respectively. -
c-Met/HGFR inhibitor
TAS-115 mesylate is a potent VEGFRand hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor, with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively. -
Raf/VEGFR3 inhibitor
Sorafenib D3 (Bay 43-9006 D3) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively. -
Raf/VEGFR3 inhibitor
Sorafenib D4 (Bay 43-9006 D4) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively. -
VEGFR-2 Inhibitor
VEGFR-2-IN-39 is a potent inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2), with an IC50 of 208.6 nM. This compound effectively inhibits the proliferation of EA.hy926 cells, a human umbilical vein endothelial cell line, in a concentration-dependent manner, exhibiting an IC50 of 38.65 µM. VEGFR-2-IN-39 has low toxicity, making it suitable for further research applications in angiogenesis and vascular biology. -
PDGFRβ/VEGFR-2 inhibitor
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. -
VEGFR2 inhibitor
VEGFR2-IN-2 (compound 6e) is a highly potent and selective inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2), exhibiting an IC50 of 19.32 nM. It effectively targets VEGFR2-mediated signaling, which is critical for tumor angiogenesis, thereby inhibiting tumor growth and metastasis. VEGFR2-IN-2 is a valuable tool for research into anti-angiogenic therapies, particularly for cancers such as colorectal, breast, lung, and ovarian cancers, where VEGFR2-driven angiogenesis plays a significant role. Its high selectivity and potency make it suitable for studying VEGFR2-specific mechanisms in tumor progression and evaluating combination therapies with other targeted agents. -
VEGFR-3 inhibitor
EVT801 is an orally active, selective VEGFR-3 inhibitor (IC50=11 nM) with potent antitumor properties. It suppresses VEGF-C-induced human endothelial cell proliferation and tumor-associated lymphatic angiogenesis in mouse models. EVT801 reduces tumor hypoxia, immunosuppressive cytokines (CCL4, CCL5), and myeloid-derived suppressor cell (MDSC) production. When combined with immune checkpoint therapy (ICT), EVT801 enhances response rates and improves tumor inhibition in cancer mouse models. Additionally, EVT801 is a click chemistry reagent containing an alkyne group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules. -
Aurora A/B inhibitor
Tinengotinib (TT00420) is an orally bioavailable, spectrally selective small-molecule kinase inhibitor targeting Aurora A/B (IC50=1.2–3.3 nM), FGFR1/2/3 (IC50=1.5–3.5 nM), VEGFRs, JAK1/2, and CSF1R. It disrupts Aurora kinase-mediated cell cycle progression, inducing G2/M arrest, inhibits the FGFR/JNK-JUN signaling pathway, and activates the MEK/ERK-dependent apoptotic pathway. Tinengotinib exhibits potent anti-tumor proliferation, pro-apoptotic, anti-angiogenic, and tumor microenvironment-modulating activities. It is a promising candidate for research in triple-negative breast cancer (TNBC), gallbladder cancer, and tumor immune microenvironment studies. -
Multi-target Inhibitor
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. -
VEGFR-2 Inhibitor
VEGFR-2-IN-77 is a selective inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2), displaying an IC50 value of 139 nM. This compound effectively disrupts the PI3K/AKT/mTOR signaling pathway, leading to cytotoxic effects specifically in leukemia and prostate cancer cells. VEGFR-2-IN-77 induces cell cycle arrest and apoptosis while inhibiting cell migration and invasion. It serves as a valuable tool for investigating therapeutic strategies in leukemia and prostate cancer research. -
VEGFR Inhibitor
Gamabufotalin is a selective inhibitor of the Vascular Endothelial Growth Factor Receptor (VEGFR). This compound, derived from the traditional Chinese medicine Chansu, exhibits potent anti-cancer properties by significantly suppressing cancer cell proliferation and modulating inflammatory responses. Its ability to inhibit angiogenesis is primarily attributed to the blockade of VEGFR-2 signaling pathways, making it a valuable tool for research in cancer therapies and vascular biology. -
VEGFR Inhibitor
Chloropyramine hydrochloride is an H1 histamine receptor antagonist that also serves as an inhibitor of vascular endothelial growth factor receptor 3 (VEGFR-3) and focal adhesion kinase (FAK). This compound exhibits key biological activities, contributing to research in angiogenesis and related pathways. It is valuable for studies aimed at understanding the role of VEGFR signaling in various physiological and pathological processes. -
EGFR/VEGFR2 Inhibitor
EGFR/VEGFR2-IN-4 is an irreversible inhibitor targeting the epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor 2 (VEGFR-2). It exhibits potent inhibitory activity with IC50 values of 18.7 nM for EGFR and 102.3 nM for VEGFR-2 in the presence of 1 μM ATP. This compound is valuable for research applications focused on cancer therapeutics and angiogenesis, providing insights into signaling pathways and potential treatment strategies. -
VEGFR iInhibitor
ZM-306416 hydrochloride is a potent inhibitor of vascular endothelial growth factor receptor (VEGFR), demonstrating IC50 values of 0.1 μM for KDR and 2 μM for Flt. In addition, it functions as an epidermal growth factor receptor (EGFR) inhibitor with an IC50 of less than 10 nM. This dual inhibition profile makes ZM-306416 hydrochloride valuable for research in cancer biology and angiogenesis, providing insights into tumor growth and vascular development mechanisms. -
VEGFR Inhibitor
Jaceidin is a selective vascular endothelial growth factor receptor (VEGFR) inhibitor that demonstrates significant anti-tumor activity. This compound is characterized by its excellent membrane permeability and oral bioavailability, making it a valuable candidate for further research. Jaceidin holds potential for applications in cancer therapy, particularly in inhibiting angiogenesis associated with tumor growth. -
EGFR/VEGFR-2 Inhibitor
EGFR-IN-121 is a potent dual inhibitor targeting EGFR and VEGFR-2, exhibiting IC50 values of 84 nM and 3.5 nM, respectively. This compound demonstrates significant biological activity that can impede tumor growth and angiogenesis by inhibiting key signaling pathways associated with cancer progression. EGFR-IN-121 is suitable for research applications focused on cancer therapeutics, particularly in evaluating the effects of EGFR and VEGFR-2 inhibition in various cancer models. -
VEGFR-2/DHFR Inhibitor
VEGFR-2/DHFR-IN-2 is a dual inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2) and Dihydrofolate Reductase (DHFR), exhibiting IC50 values of 0.623 μM and 9.085 μM, respectively. This compound demonstrates significant cytotoxic activity against various cancer cell lines, including C26, HepG2, and MCF7, with IC50 values ranging from 3.59 to 8.38 μM. VEGFR-2/DHFR-IN-2 is pertinent for research applications focused on cancer therapeutics and targeted inhibition of tumor angiogenesis. -
VEGFR-2/DHFR Inhibitor
VEGFR-2/DHFR-IN-1 is a dual inhibitor of VEGFR-2 and dihydrofolate reductase (DHFR), exhibiting IC50 values of 0.384 μM and 7.881 μM, respectively. This compound demonstrates significant antibacterial activity against various strains, including Escherichia coli and MRSA, with MIC values ranging from 8 to 16 μg/mL. Additionally, VEGFR-2/DHFR-IN-1 shows potent cytotoxic effects on cancer cell lines C26, HepG2, and MCF7, with IC50 values between 2.97 and 7.12 μM. This reagent is applicable for research exploring cancer therapeutics and microbial resistance. -
VEGFR inhibitor
NVP-BAW2881 is a potent and selective VEGFR inhibitor (vascular endothelial growth factor receptor tyrosine kinase inhibitor) with activity to inhibit chronic and acute skin inflammation. -
c-Met/VEGFR inhibitor
Altiratinib is a novel c-MET/TIE-2/VEGFR inhibitor; effectively reduce tumor burden in vivo and block c-MET pTyr(1349)-mediated signaling, cell growth and migration as compared with a HGF antagonist in vitro. -
VEGFR inhibitor
Fruquintinib is an orally available, small molecule inhibitor of vascular endothelial growth factor receptors (VEGFRs), with potential anti-angiogenic and antineoplastic activities. -
VEGF and PDGF inhibitor
Ningetinib Tosylate,also known as CT-053Tosylate and DE-120, is a VEGF and PDGF inhibitor potentially for the treatment of wet age-related macular degeneration. CAS: 1394820-69-9 (free base) 1394820-77-9 (tosylate) -
tyrosine kinase inhibitor
Ningetinib is a multi-kinase inhibitor that inhibits c-Met, VEGFR2/KDR, and Axl with IC50s value of 19, 37, and 11 nM, respectively. -
RTK inhibitor
Anlotinib, also known as AL3818, is a receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic and anti-angiogenic activities. CAS: 1058156-90-3 (free base) 1360460-82-7 (HCl)
