Catalog No.
Product Name
Application
Product Information
Citations
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VEGFR2 Inhibitor
VEGFR-2-IN-35 is a potent inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2), exhibiting an IC50 value of 37 nM. This compound demonstrates significant anti-proliferative effects on MCF-7 and HCT 116 cancer cell lines, with IC50 values of 10.56 µM and 7.07 µM, respectively. VEGFR-2-IN-35 is suitable for research applications focused on angiogenesis and cancer cell proliferation. -
hCA/VEGFR-2 Inhibitor
hCA/VEGFR-2-IN-3 is a potent inhibitor targeting cancer-associated human carbonic anhydrases (hCAs) IX and XII, as well as vascular endothelial growth factor receptor 2 (VEGFR-2). It demonstrates a VEGFR-2 inhibition with an IC50 of 358 nM and shows strong binding affinity to hCA IX with a Ki of 4.2 nM, as well as significant binding to hCA II, hCA I, and hCA XII. This compound exhibits antiproliferative properties in VEGFR-2-overexpressing breast cancer cells, making it valuable in cancer research and potential therapeutic applications. -
VEGFR-1
AGN-745 is a chemically modified siRNA designed to specifically target Vascular Endothelial Growth Factor Receptor 1 (VEGFR-1). This reagent plays a crucial role in the study of macular degeneration by inhibiting the expression of VEGFR-1, which is involved in angiogenesis and vascular permeability. It serves as a valuable tool for researchers investigating therapeutic interventions for retinal diseases linked to abnormal vascularization. -
EGFR Inhibitor
EGFR-IN-26 is a selective inhibitor of the epidermal growth factor receptor (EGFR), derived from patent WO2019162323A1, compound I-028. This compound significantly impedes EGFR activity, making it a valuable tool for investigating its role in cancer biology. It is applicable in cancer research, particularly in studies focused on targeting EGFR signaling pathways to develop novel therapeutic strategies. -
VEGFR Inhibitor
ZD-4190 hydrochloride is a potent inhibitor of Vascular Endothelial Growth Factor Receptor (VEGFR), demonstrating significant anti-tumor activity. This compound effectively inhibits tumor cell proliferation and angiogenesis, leading to delayed growth of MDA-MB-435 tumors. ZD-4190 hydrochloride is valuable for research on cancer therapeutics and the exploration of VEGFR signaling pathways. -
VEGFR Inhibitor
Vatalanib succinate is a potent orally active inhibitor of vascular endothelial growth factor receptors (VEGFR), specifically targeting KDR with an IC50 of 37 nM. Inhibition of additional receptors, including Flt-1, Flk, Flt-4, c-Kit, c-Fms, and PDGFR-β, is observed at various IC50 values, ranging from 77 nM to 1400 nM. This compound is primarily utilized in research applications focusing on angiogenesis, cancer treatment, and vascular biology studies. -
VEGFR2 Inhibitor
VEGFR-2-IN-17 is a potent inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2), exhibiting an IC50 of 67.25 nM. This compound demonstrates significant antitumor activity, making it a valuable tool for studying angiogenesis and tumor progression. VEGFR-2-IN-17 is suitable for research applications focused on cancer biology and the development of anti-angiogenic therapies. -
TIE-2/VEGFR-2 Inhibitor
TIE-2/VEGFR-2 kinase-IN-5 is a selective inhibitor of TIE-2 and VEGFR-2 receptor tyrosine kinases, with reported pIC50 values of 7.78 nM and 8.11 nM, respectively. This compound exhibits strong anti-angiogenic properties, making it valuable for studies investigating angiogenesis and associated therapeutic strategies. Its ability to effectively disrupt signaling pathways involved in blood vessel formation positions TIE-2/VEGFR-2 kinase-IN-5 as a critical tool for research in vascular biology and cancer therapeutics. -
FLuc/VEGFR Inhibitor
GW549390X is a dual inhibitor targeting FLuc and VEGFR2, demonstrating IC50 values of 0.26 μM and 1.2 μM, respectively. It functions as an ATP-competitive inhibitor of FLuc by binding to the ATP pocket via its aniline side chain. This compound serves as a protein kinase inhibitor, providing utility in various assays involving ATP-dependent and -independent luciferases, making it relevant for research in signal transduction and cancer biology. -
VEGFR Inhibitor
PF-00337210 is a potent and selective inhibitor of Vascular Endothelial Growth Factor Receptors (VEGFRs). This compound is primarily investigated for its therapeutic application in age-related macular degeneration, aiming to provide sustained drug delivery through a unique ophthalmic solution that forms a depot upon intravitreal injection. Its development addresses critical challenges such as maintaining low dosing volumes, ensuring safety for intravitreal use, and optimizing physicochemical properties, resulting in a stable, isotonic formulation suitable for prolonged release in ocular tissues. -
HIF-1α Inhibitor
7-Hydroxyneolamellarin A is a potent inhibitor of hypoxia-inducible factor-1α (HIF-1α), a key regulator of cellular responses to low oxygen levels. Derived from the sponge Dendrilla nigra, this natural product effectively reduces HIF-1α protein accumulation and suppresses its transcriptional activity on vascular endothelial growth factor (VEGF). Research applications of 7-Hydroxyneolamellarin A include investigations into cancer biology and the modulation of tumor microenvironments. -
VEGFR-2 Inhibitor
VEGFR-2-IN-27 is a potent inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2), displaying an IC50 value of 14.8 nM. This compound is primarily utilized in research focused on the mechanisms of angiogenesis and tumor growth. Its application in anticancer studies provides valuable insights into targeting vascular pathways for therapeutic intervention. -
VEGFR Inhibitor
AG-28262 is a potent VEGFR inhibitor, primarily targeting vascular endothelial growth factor receptors to impede angiogenesis. This compound exhibits significant anti-angiogenic activity, making it a valuable tool for research in cancer therapies and other conditions related to abnormal blood vessel formation. Its application is particularly relevant in studies focusing on tumor progression and metastasis, offering insights into therapeutic strategies that can inhibit tumor-related angiogenesis. -
VEGFR2 Inhibitor
(E)-FeCP-oxindole is a selective inhibitor of the human vascular endothelial growth factor receptor 2 (VEGFR2) with an IC50 value of 200 nM. This compound also exhibits significant inhibitory effects on VEGFR1 and PDGFRα/β at concentrations of 10 μM. Additionally, (E)-FeCP-oxindole demonstrates notable anticancer activity, particularly against B16 murine melanoma lines, with an IC50 of less than 1 μM, making it a valuable reagent for cancer research and vascular biology studies. -
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. -
PDGFR Inhibitor
cis-SU4312 is a potent inhibitor of the Platelet-Derived Growth Factor Receptor (PDGFR) and FLK-1, exhibiting IC50 values of 19.4 μM and 0.8 μM, respectively. Additionally, cis-SU4312 targets several other receptors, including EGFR, HER-2, and IGF-1R with IC50 values of 24.2 μM, 18.5 μM, and 10.0 μM, respectively. Due to its ability to cross the blood-brain barrier, cis-SU4312 is valuable in research applications related to cancer biology and neurobiology. -
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.
