Catalog No.
Product Name
Application
Product Information
Citations
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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. - Oglufanide inhibits vascular endothelial growth factor (VEGF), which may inhibit angiogenesis. This agent has also been reported to stimulate the immune response to hepatitic C virus and intracellular bacterial infections.
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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/c-Met/HGFR inhibitor
TAS-115 is a potent VEGFR and hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively. -
multi-targeted kinase inhibitor
ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively. -
VEGFR inhibitor
Cediranib maleate (AZD-2171 maleate) is a highly potent, orally available VEGFR inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively. -
VEGFR2/KDR inhibitor
Vatalanib (PTK787; ZK-222584; CGP-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM. -
tyrosine kinase inhibitor
Sulfatinib (HMPL-012) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC50s of in a range of 1 to 24 nM. -
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. - ATWLPPR peptide is a biologically active heptapeptide and a specific antagonist of VEGFR2 (KDR/Flk-1). It binds to VEGFR2, completely blocking VEGF binding and thereby inhibiting VEGF-induced angiogenesis in vivo. ATWLPPR selectively inhibits human endothelial cell proliferation in vitro and fully suppresses VEGF-mediated angiogenesis in vivo.
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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-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. -
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-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. -
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 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. -
VEGFR2/MET Inhibitor
Cabozantinib hydrochloride is a potent inhibitor of VEGFR2 and MET, exhibiting IC50 values of 0.035 nM and 1.3 nM, respectively. Additionally, it effectively inhibits other receptor tyrosine kinases including KIT, RET, AXL, TIE2, and FLT3 with IC50 values of 4.6 nM, 5.2 nM, 7 nM, 14.3 nM, and 11.3 nM. This compound demonstrates significant antiangiogenic properties by disrupting tumor vasculature and inducing apoptosis in both tumor and endothelial cells. It is widely utilized in cancer research to explore the mechanisms of tumor progression and treatment resistance. -
c-kit/VEGFR/PDGFR Inhibitor
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. -
VEGFR2/KDR Inhibitor
Vatalanib hydrochloride is a potent and selective inhibitor of VEGFR2 (vascular endothelial growth factor receptor 2), with an IC50 of 37 nM. It effectively penetrates the blood-brain barrier, making it suitable for studies involving central nervous system applications. Vatalanib hydrochloride is utilized in research focused on angiogenesis, tumor growth inhibition, and vascular biology, contributing valuable insights into therapeutic strategies for various cancers. -
VEGFR-2 Inhibitor
VEGFR-2-IN-15 is a selective inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2), a key regulator of angiogenesis. This compound effectively arrests cell growth in HepG2 cells at the Pre-G1 phase and induces apoptosis. It is a valuable tool for research applications focused on cancer biology and therapeutic strategies targeting angiogenesis. -
c-kit/VEGFR/PDGFR Inhibitor
Famitinib is a potent multi-targeted kinase inhibitor that primarily targets c-kit, VEGFR-2, and PDGFRβ, with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively. This orally active compound demonstrates significant antitumor activity in human gastric cancer cells and xenograft models. Famitinib also induces apoptosis, making it a valuable tool for research in cancer therapeutics and signaling pathways. -
VEGFR2 Inhibitor
JK-P3 is a selective inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) with IC50 values of 7.83 μM for VEGFR2, 27 μM for FGFR1, and 5.18 μM for FGFR3. It effectively blocks VEGF-A-induced VEGFR2 activation and downstream signaling pathways, demonstrating inhibition of endothelial cell migration and angiogenesis in vitro. Additionally, JK-P3 suppresses fibroblast growth factor receptor kinase activity, contributing to its anti-angiogenic properties and making it a valuable tool for research in vascular biology and cancer therapeutics. -
VEGFR/FGFR Inhibitor
Lucitanib dihydrochloride is a selective dual inhibitor targeting VEGFR and FGFR, demonstrating potent inhibition of VEGFR1, VEGFR2, VEGFR3, FGFR1, and FGFR2 with IC50 values of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively. This inhibitor plays a critical role in regulating angiogenesis and tumor growth, making it valuable for research in cancer biology and therapeutic development. Lucitanib dihydrochloride is suitable for studies focused on vascular endothelial growth factor signaling pathways and fibroblast growth factor signaling, contributing to the understanding of tumor microenvironment interactions. -
VEGFR-2/FGF Inhibitor
CP-547632 TFA is a potent, orally active inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2) and Fibroblast Growth Factor (FGF) kinases, exhibiting IC50 values of 11 nM and 9 nM, respectively. This reagent demonstrates notable selectivity for VEGFR-2 and bFGF over other tyrosine kinases, including EGFR and PDGFRβ. CP-547632 TFA is primarily utilized in cancer research due to its antitumor efficacy, making it a valuable tool for studies focused on angiogenesis and tumor development. -
VEGFR-2 And FGFR-1 Inhibitor
BMS-645737 is a selective inhibitor of FGF receptor-1 (FGFR-1) and VEGF receptor-2 (VEGFR-2), acting through competitive inhibition of their tyrosine kinase activity. It exhibits potent anti-angiogenic properties, making it a valuable tool in cancer research and studies related to tumor-induced angiogenesis. Additionally, BMS-645737 has been observed to induce lesions in incisor teeth, further highlighting its potential for studying tissue effects and side effects in therapeutic contexts. -
ALK/IR/VEGFR2/TIE2/DLK Inhibitor
CEP-14083 is an ATP-competitive inhibitor targeting ALK, with IC50 values of 2 nM in enzymatic assays. This compound also inhibits other kinases, including the insulin receptor (IR), vascular endothelial growth factor receptor 2 (VEGFR2), angiopoietin-1 receptor (TIE2), and dual leucine zipper kinase (DLK). CEP-14083 has been shown to suppress CD274 mRNA expression and the function of NPM/ALK in NPM/ALK-positive T cell lymphoma cells. It is a valuable tool for research focused on lymphoma and related signaling pathways.
