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VEGFR2 Inhibitor
YF-452 is a potent inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2). It effectively disrupts the migration, invasion, and tube-like structure formation of human umbilical vein endothelial cells (HUVECs) while exhibiting minimal toxicity. YF-452 inhibits VEGF-induced phosphorylation of VEGFR2 and downstream signaling pathways, including extracellular signal-regulated kinase (ERK), focal adhesion kinase (FAK), and Src. This compound represents a promising candidate for antiangiogenic research in cancer studies. -
VEGFR Inhibitor
AG-13958 (mono(hydrochloride)) is a selective inhibitor of vascular endothelial growth factor receptor (VEGFR) tyrosine kinases. It demonstrates significant biological activity in inhibiting angiogenesis and has been investigated for its potential therapeutic applications in conditions such as choroidal neovascularization linked to age-related macular degeneration (AMD). This compound serves as a valuable tool in research focusing on the modulation of angiogenic pathways. -
VEGFR2 Inhibitor
VEGFR2-IN-3 is a selective inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2), which plays a crucial role in angiogenesis and vascular permeability. This compound demonstrates significant antiproliferative activity against endothelial cells and is valuable in studying tumor growth and metastasis mechanisms. VEGFR2-IN-3 is useful for research applications aimed at understanding and targeting angiogenic pathways in cancer therapy. -
BRAF/VEGFR2 Inhibitor
Takeda-6D is a potent and orally active inhibitor targeting BRAF and VEGFR2, displaying IC50 values of 7.0 nM and 2.2 nM, respectively. This compound effectively suppresses angiogenesis by inhibiting the VEGFR2 signaling pathway in 293/KDR and VEGF-stimulated HUVEC cells. Additionally, Takeda-6D demonstrates significant inhibition of ERK1/2 phosphorylation, indicating its potential for antitumor activity in various cancer research applications. -
VEGFR Inhibitor
NVP-AAD777 is a selective inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2) that effectively suppresses phospho-VEGFR-2 (Tyr1175) signaling. In animal studies, NVP-AAD777 demonstrated a lack of adverse effects on lung architecture and vascular density, even when used alongside cigarette smoke exposure. This profile underscores its potential as a therapeutic agent for conditions related to dysregulated VEGFR-2 signaling, promoting vascular integrity without detrimental pulmonary consequences. -
VEGFR Inhibitor
DW10075 is a selective VEGFR inhibitor that targets the VEGF/VEGFR signaling pathway, effectively inhibiting VEGFR-1, VEGFR-2, and VEGFR-3 without affecting FGFR or PDGFR. This compound demonstrates significant biological activity by inhibiting VEGF-induced proliferation, migration, and tube formation in human umbilical vein endothelial cells (HUVECs). Additionally, DW10075 effectively suppresses angiogenesis in the rat aortic ring and chick chorionic membrane models. It exhibits antiproliferative effects against various human cancer cell lines, showing IC50 values of 2.2 μM for U87-MG glioblastoma cells and 22.2 μM for A375 melanoma cells, with notable tumor growth inhibition in the nude mouse U87-MG xenograft model. -
VEGFR2 Inhibitor
VEGFR2-IN-1 is a potent and selective inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR2), with an IC50 value of 19.8 nM. This compound effectively inhibits cell proliferation and migration by promoting apoptosis through its action on VEGFR2. VEGFR2-IN-1 is suitable for research applications focused on cancer biology, angiogenesis, and the therapeutic targeting of vascular pathways. -
hCA/VEGFR-2 Inhibitor
hCA/VEGFR-2-IN-4 is an indolinylbenzenesulfonamide that acts as a dual inhibitor of human carbonic anhydrases (hCAs) IX and XII, as well as vascular endothelial growth factor receptor 2 (VEGFR-2). This compound demonstrates potent inhibition of VEGFR-2 with an IC50 of 0.811 μM and exhibits significant binding affinity to hCAs, with Ki values of 3.8 nM for hCA XII, 6.2 nM for hCA IX, 19.8 nM for hCA II, and 35.5 nM for hCA I. Additionally, hCA/VEGFR-2-IN-4 shows antiproliferative effects on breast cancer cells that overexpress VEGFR-2, making it a valuable tool for cancer research. -
VEGFR2 Tyrosine Kinase Inhibitor
YM-359445 dihydroxybutanedioate is an orally active inhibitor targeting the VEGFR2 tyrosine kinase, exhibiting an IC50 of 8.5 nM. This compound effectively inhibits vascular permeability induced by VEGF, demonstrating significant potential in modulating angiogenesis. Additionally, YM-359445 dihydroxybutanedioate exhibits antitumor activity against lung cancer as well as Paclitaxel-resistant colon cancer, making it a valuable reagent for cancer research applications. -
hCA/VEGFR-2 Inhibitor
hCA/VEGFR-2-IN-2 is an indolinonylbenzenesulfonamide functioning as a dual inhibitor targeting cancer-associated human carbonic anhydrases (hCAs) IX and XII, as well as vascular endothelial growth factor receptor 2 (VEGFR-2). The compound exhibits potent inhibitory activity against VEGFR-2 with an IC50 of 204 nM, and demonstrates high affinity for hCAs with inhibition constants of 3.6 nM for hCA IX, 16.1 nM for hCA II, 16.7 nM for hCA XII, and 75.3 nM for hCA I. This compound also displays antiproliferative effects on breast cancer cells that overexpress VEGFR-2, making it a valuable tool in cancer research and therapeutic development. -
VEGFR Inhibitor
Bevasiranib is a small interfering RNA (siRNA) that specifically targets the genes responsible for producing vascular endothelial growth factor (VEGF). By inhibiting VEGF synthesis, bevasiranib plays a critical role in addressing choroidal neovascularization (CNV), which is a significant contributor to the development of wet age-related macular degeneration (wet AMD). This compound is essential for researchers aiming to investigate therapeutic strategies for vascular-related eye diseases. -
FLuc/VEGFR Inhibitor
GW809897X is a dual inhibitor of firefly luciferase (Fluc) and vascular endothelial growth factor receptor (VEGFR), exhibiting IC50 values of 0.58 μM and 65 nM, respectively. This compound serves as a protein kinase inhibitor, influencing both ATP-dependent and -independent luciferase activities. Its efficacy makes it valuable for applications involving Fluc reporter assays and investigations into VEGFR-mediated signaling pathways. -
VEGFR Inhibitor
VEGFR-2-IN-10 is a selective inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2), demonstrating significant antiangiogenic activity with an IC50 of 0.7 μM against VEGF-induced VEGFR-2 phosphorylation. This compound effectively blocks the signaling pathways that promote angiogenesis without inducing cytotoxic effects. VEGFR-2-IN-10 is ideal for researchers investigating the mechanisms of angiogenesis and its role in various pathological conditions, including cancer. -
VEGFR Inhibitor
YLT192 is a potent VEGFR2 inhibitor with significant anti-angiogenic and anti-tumor properties. It effectively inhibits the kinase activity of VEGFR2, resulting in decreased proliferation, migration, invasion, and tube formation of human umbilical cord vascular endothelial cells. Additionally, YLT192 disrupts VEGF-induced VEGFR2 phosphorylation and its downstream signaling pathways. In vivo studies using zebrafish embryo models and alginate-coated tumor cell assays have demonstrated its capability to inhibit angiogenesis while also promoting apoptosis in various cancer cell lines. -
VEGFR2 Inhibitor
VEGFR-2-IN-16 is a selective inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2) with an IC50 of 86.36 nM. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. It is suitable for studies aimed at elucidating the role of VEGFR-2 in tumor angiogenesis and exploring therapeutic strategies in oncology. -
VEGFR Inhibitor
SU5208 is a selective inhibitor of vascular endothelial growth factor receptor-2 (VEGFR2). By blocking VEGFR2 signaling, SU5208 effectively impedes angiogenesis and tumor growth, making it a valuable tool in cancer research. Its ability to modulate vascular endothelial cell proliferation and migration supports its applications in studying tumor vasculature and related pathological conditions. -
Anti-VEGFR2/KDR/CD309 Antibody
Girancitug is a humanized IgG1κ monoclonal antibody that specifically targets the vascular endothelial growth factor receptor 2 (VEGFR2/KDR/CD309). It effectively inhibits angiogenesis, making it a valuable tool in cancer research. Girancitug is applicable in anti-angiogenic therapy studies, particularly for cancers such as colorectal and ovarian cancers. -
VEGFR Inhibitor
CEP-7055 is a selective vascular endothelial growth factor receptor 2 (VEGFR-2) tyrosine kinase inhibitor that demonstrates potent low nanomolar inhibition of human VEGFR-2. This compound shows enhanced selectivity against various tyrosine and serine/threonine kinases, making it a suitable tool for investigating angiogenesis and tumor growth. In vivo studies have confirmed notable antitumor effects across multiple tumor models, and CEP-7055 has advanced into phase I clinical trials as a prodrug designed to improve water solubility and oral bioavailability through its N,N-dimethylglycine ester formulation. -
VEGFR Inhibitor
CPD-002 is a selective inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2), targeting the VEGFR2/PI3K/AKT signaling pathway to inhibit angiogenesis. In addition to its anti-angiogenic properties, CPD-002 demonstrates significant anti-inflammatory activity, making it a valuable tool for research in conditions such as rheumatoid arthritis. This reagent is ideal for investigating the roles of VEGFR2 in various biological processes and therapeutic applications. -
FLuc/VEGFR Inhibitor
GW701427A is a dual inhibitor targeting Fluc and VEGFR2, exhibiting IC50 values of 0.12 μM and 603 nM, respectively. This compound functions as a protein kinase inhibitor, affecting both ATP-dependent and -independent luciferases. GW701427A is valuable for research applications involving Fluc reporter assays and studies on angiogenesis and vascular signaling pathways. -
VEGFR Inhibitor
CEP-5214 is a potent inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2) tyrosine kinase, derived from an indenopyrrolocarbazole template. With an IC50 value of 8 nM against VEGF-R2, it demonstrates remarkable selectivity over other kinases, exhibiting low-nanomolar inhibition (IC50 of 4 nM). This compound has shown significant antitumor activity in both cellular and in vivo models, and it has advanced to phase I clinical trials in the form of a water-soluble prodrug (CEP-7055) to improve oral bioavailability. Its distinctive mechanism of action makes it valuable for research applications related to cancer and angiogenesis. -
VEGFR Inhibitor
VEGFR-2-IN-20 is a potent inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2). This compound exhibits strong anti-angiogenic activity, making it a valuable tool for investigating mechanisms of tumor growth and metastasis in cancer research. It is particularly useful for studies focused on targeting VEGFR signaling pathways in various malignancies. -
VEGFR-2 Inhibitor
VEGFR-2-IN-26 is a highly potent inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2), demonstrating an IC50 value of 15.5 nM. This compound exhibits significant antiproliferative activity across various cancer cell lines, including leukemic, non-small cell lung, CNS, ovarian, renal, prostate, and breast cancers. VEGFR-2-IN-26 serves as a valuable tool for cancer research, particularly in studies targeting tumor angiogenesis and metastasis. -
TIE-2/VEGFR-2 Inhibitor
TIE-2/VEGFR-2 kinase-IN-3 is a benzimidazole compound that selectively inhibits TIE-2 and VEGFR-2 tyrosine kinase receptors, exhibiting IC50 values of 6.9 nM and 3.5 nM, respectively. This inhibitor is valuable for research focused on angiogenesis, providing insights into tumor growth and vascular development. Its potent activity makes it a significant tool for investigating therapeutic strategies targeting vascular-related diseases. -
TIE-2/VEGFR-2 Inhibitor
TIE-2/VEGFR-2 kinase-IN-4 is a benzimidazole compound that functions as a potent inhibitor of TIE-2 and VEGFR-2 tyrosine kinase receptors, with IC50 values of 5.2 nM and 5.1 nM, respectively. This inhibitor effectively modulates signaling pathways involved in angiogenesis, making it a valuable reagent for research focused on vascular development and tumor growth. Its specificity for both targets allows for detailed studies in cancer biology and therapeutic development. -
PROTAC VEGFR2 Degrader
PROTAC VEGFR-2 Degrader-1 is a targeted protein degradation compound designed to selectively degrade VEGFR-2. It demonstrates minimal VEGFR-2 inhibition with an IC50 exceeding 1 μM, and exhibits limited anti-proliferative activity against EA.hy926 cells, with an IC50 greater than 100 μM. This reagent is valuable for research applications focused on the regulation of VEGFR-2 and its role in vascular biology and related disease mechanisms. -
VEGFR-2/c-Met Inhibitor
VEGFR-2/c-Met-IN-1 is a potent dual inhibitor targeting vascular endothelial growth factor receptor 2 (VEGFR-2) and c-Met, with IC50 values of 138 nM and 74 nM, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its dual mechanism of action allows for the exploration of therapeutic strategies aimed at inhibiting tumor growth and angiogenesis. -
VEGFR-2 Inhibitor
VEGFR-2-IN-25 is a potent inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2), exhibiting an IC50 value of 12.1 nM. This compound is primarily utilized in cancer research to investigate the role of angiogenesis in tumor progression and to evaluate therapeutic strategies targeting the VEGF signaling pathway. Its efficacy makes it a valuable tool for studying anti-tumor effects in various cancer models. -
PROTAC VEGFR2 Degrader
PROTAC VEGFR-2 Degrader-2 primarily targets the vascular endothelial growth factor receptor 2 (VEGFR-2) for degradation through the PROTAC mechanism. This compound displays minimal inhibition of VEGFR-2 activity with an IC50 exceeding 1 μM and demonstrates anti-proliferative effects in EA.hy926 cells, with an IC50 greater than 100 μM. It serves as a valuable tool for studies focused on targeted protein degradation and the modulation of signaling pathways related to angiogenesis. -
VEGFR-2 Inhibitor
VEGFR-2-IN-24 is a potent inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2), exhibiting an IC50 value of 0.22 µM. This compound is valuable in tumor research, facilitating the study of angiogenesis and the role of VEGFR-2 in various cancer models. Its efficacy makes it a useful tool for investigating therapeutic strategies targeting tumor vascularization. -
VEGFR-2 Inhibitor
VEGFR-2-IN-65 is a selective inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2). It demonstrates high affinity and forms hydrogen bond interactions with Cys180 of the receptor. This compound has been shown to effectively inhibit tube formation in human umbilical vein endothelial cells (HUVECs), making it a valuable tool for investigating angiogenesis and vascular biology pathways. Research applications include the study of tumor angiogenesis and vascular disorders. -
FLuc/VEGFR Inhibitor
GSK248233A is a dual inhibitor targeting FLuc and VEGFR2, exhibiting IC50 values of 1.03 μM and 2 nM, respectively. This compound also demonstrates activity against the AGC family of protein kinases. By inhibiting ATP-dependent and -independent luciferases, GSK248233A holds potential for applications in FLuc reporter assays and related biological research. -
VEGFR Inhibitor
VEGFR-IN-7 is a selective inhibitor of Vascular Endothelial Growth Factor Receptor (VEGFR), primarily involved in regulating angiogenesis. This compound demonstrates potential for modulating angiogenic processes and is particularly relevant in the study of cardiovascular diseases and related pathologies. Its ability to interfere with VEGFR signaling makes it a valuable tool for investigating therapeutic strategies aimed at vascular-related conditions. -
VEGFR Inhibitor
VEGFR/PDGFR-IN-1 is a potent inhibitor of the Vascular Endothelial Growth Factor Receptor (VEGFR) with an IC50 of 0.4 μM. This compound effectively inhibits angiogenesis in Human Umbilical Vein Endothelial Cells (HUVEC), demonstrating potential for application in tumor growth and metastasis research. Its targeted mechanism makes it a valuable tool for studying vascular-related pathologies and developing anti-cancer therapies. -
SRC/Raf/VEGFR2 Inhibitor
SKLB646 is a multi-target kinase inhibitor with a focus on SRC, Raf, and VEGFR2. It exhibits potent inhibitory activity against SRC and VEGFR2, with IC50 values of 0.002 μmol/L and 0.012 μmol/L, respectively, as well as significant effects on B-Raf and C-Raf. SKLB646 disrupts SRC signaling and inhibits the MAPK pathway by targeting Raf kinases, leading to decreased proliferation, migration, and invasion in human umbilical vein endothelial cells (HUVEC), thereby impeding tumor-induced angiogenesis. It also demonstrates significant anti-proliferative and anti-survival effects on triple-negative breast cancer (TNBC) cell lines, making it a valuable tool for cancer research. -
VEGFR Antagonist
K-106 is a selective vascular endothelial growth factor receptor (VEGFR) antagonist that also inhibits neurotrophic tyrosine kinase receptors (NTRK). This compound exhibits significant biological activity in modulating angiogenesis and neuroprotection, making it a valuable tool for investigating retinal research and related therapeutic applications. Its dual inhibitory profile supports studies focused on vascular and neurological disorders. -
VEGFR Inhibitor
VEGFR-IN-6 is an inhibitor of the vascular endothelial growth factor receptor (VEGFR), known for its ability to impede angiogenesis. This compound is particularly relevant in the study of tumor biology, where angiogenesis plays a critical role in tumor progression and metastasis. VEGFR-IN-6 serves as a valuable tool for researchers investigating the mechanisms of cancer and the development of anti-angiogenic therapies. -
VEGFR2 Kinase Inhibitor
VEGFR2-IN-4 is a selective inhibitor of the VEGFR2 kinase, exhibiting a GI50 value of 0.7 nM. This compound demonstrates significant anti-angiogenic activity, making it a valuable tool for investigating the role of angiogenesis in various biological processes. VEGFR2-IN-4 is suitable for research applications related to rheumatoid arthritis and other angiogenesis-associated conditions. -
VEGFR2/FAK Inhibitor
ZINC09875266 is a dual inhibitor that specifically targets Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) and Focal Adhesion Kinase (FAK). This compound demonstrates potent inhibitory activity that can suppress angiogenesis and cancer cell proliferation. Research applications include studying tumor growth and metastasis in various cancer models. -
VEGFR-2/c-Met Inhibitor
Taligantinib is a selective dual inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2) and hepatocyte growth factor receptor (c-Met). This orally active compound effectively suppresses tumor angiogenesis and cell proliferation. Taligantinib is of particular interest in the research of solid tumors, including non-small cell lung cancer and hepatocellular carcinoma, making it a valuable tool for cancer biology studies. -
MET/VEGFR2/KDR Inhibitor
Foretinib phosphate is a potent inhibitor of the c-MET and VEGFR2 receptors, which play crucial roles in tumor growth and angiogenesis. By selectively targeting hepatocyte growth factor receptor c-MET and vascular endothelial growth factor receptor 2, Foretinib phosphate exhibits significant anti-tumor activity, potentially reducing tumor cell proliferation and metastasis. Its unique mechanism offers distinct advantages over other treatments, making it a valuable tool for research in oncology, particularly in studies related to lung cancer and the pathways involving MEK1/2, FER, and AURKB. -
VEGFR-2/c-Met Inhibitor
VEGFR-2/c-Met-IN-2 is a selective inhibitor targeting VEGFR-2 and c-Met, demonstrating IC50 values of 83 nM and 48 nM, respectively. This compound exhibits significant cytotoxicity against the HCT-116 cell line, with an IC50 of 3.403 µM. Its potent inhibitory effects make it a valuable tool for research into angiogenesis and cancer metastasis. -
c-Met/VEGFR-2 Inhibitor
T-1840383 is a highly potent ATP-competitive inhibitor targeting c-Met and VEGFR-2, demonstrating IC50 values of 1.9 nM for c-Met, 7.7 nM for VEGFR1, 2.2 nM for VEGFR2, and 5.5 nM for VEGFR3. This compound effectively inhibits key signaling pathways associated with cancer progression and angiogenesis. It is suitable for research applications focused on tumor growth and vascular development, making it a valuable tool in oncology and vascular biology studies. -
ALK5/VEGFR2 Inhibitor
Tosposertib is a dual inhibitor targeting ALK5 and VEGFR2, with IC50 values of 1.2 nM and 4.9 nM, respectively. This compound effectively restores the functionality of cytotoxic T lymphocytes (CTLs) and natural killer cells that are suppressed by TGFβ, while concurrently inhibiting the activity and viability of regulatory T cells. Tosposertib is valuable for research applications related to melanoma and colon cancer. -
VEGFR/PDGFα/c-Kit Inhibitor
Telatinib mesylate is a potent, orally active inhibitor of VEGFR2, VEGFR3, PDGFα, and c-Kit, exhibiting IC50 values of 6 nM, 4 nM, 15 nM, and 1 nM respectively. This compound effectively impedes angiogenesis and tumor cell proliferation, making it a valuable tool in cancer research. Its selective targeting of key signaling pathways has potential applications in studying tumor microenvironments and in developing therapeutic strategies for various malignancies. -
VEGFR Inhibitor
Tafetinib analogue 1 is a selective inhibitor of the vascular endothelial growth factor receptor (VEGFR). This compound exhibits potent anti-angiogenic activity, making it a valuable tool for investigating the role of VEGFR in tumor growth and metastasis. Tafetinib analogue 1 is applicable in cancer research, particularly in studies focusing on therapeutic strategies targeting the VEGF signaling pathway. -
EphB4, VEGFR-2 and PDGFR-β Inhibitor
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. -
VEGFR Ligand
Peptide HRH is a polypeptide that specifically targets vascular endothelial growth factor receptors (VEGFR). It effectively inhibits VEGF-stimulated endothelial cell proliferation, thereby disrupting angiogenesis. Additionally, Peptide HRH demonstrates efficacy in suppressing corneal neovascularization. This peptide is suitable for research applications focused on anti-angiogenesis and related studies. -
VEGFR2 Inhibitor
VEGFR2-IN-84 is a potent VEGFR2 inhibitor that operates as a multi-targeted tyrosine kinase inhibitor utilizing a naphthalene ring scaffold. It exhibits sub-nanomolar affinity for VEGFR2 and effectively inhibits other kinases, including Kit, FGFR, PDGFR, and Ret. By competitively binding to the ATP-binding pocket, VEGFR2-IN-84 disrupts the phosphorylation of VEGFR2, leading to significant reduction in endothelial cell proliferation, migration, and tumor angiogenesis. This compound demonstrates broad antiproliferative activity against various solid tumors, such as liver, lung, and renal cancers, while exhibiting low toxicity to normal cells. VEGFR2-IN-84 is suitable for research applications focused on malignant tumors. -
VEGFR/Tyrosine Kinase Src Inhibitor
TG 100948 is a dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and tyrosine kinase Src. This compound demonstrates significant biological activity by reducing retinal edema and retinal thickening, as well as eliminating bullous edema cysts in rat models of ischemic retinal vein occlusion. TG 100948 is valuable for research into the pathophysiology and potential treatments of ischemic retinal vein occlusion.

