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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
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. -
PDGFRβ Inhibitor
SU16f is a potent and selective inhibitor of PDGFRβ, exhibiting IC50 values of 10 nM for PDGFRβ, 140 nM for VEGF-R2, and 2.29 μM for FGF-R1. By effectively neutralizing the PDGFRβ receptor, SU16f disrupts the supportive effects of gastric cancer-derived mesenchymal stem cells (GC-MSCs) conditioned medium on gastric cancer cell proliferation and migration. This compound is valuable for research applications focused on gastric cancer and the modulation of tumor microenvironments. -
PDGFR Inhibitor
PDGFR Tyrosine Kinase Inhibitor III is a potent inhibitor of platelet-derived growth factor receptor (PDGFR), along with other kinases such as EGFR, FGFR, PKA, and PKC. This multikinase inhibitor plays a crucial role in modulating various signaling pathways involved in cellular proliferation and survival. Its application extends to the investigation of amyotrophic lateral sclerosis, providing insights into the underlying mechanisms of this neurodegenerative disorder. Researchers can employ this compound to explore therapeutic strategies targeting PDGFR and associated pathways. -
PDGFR Inhibitor
WQ-C-401 is an orally active inhibitor of the platelet-derived growth factor receptor (PDGFR), effectively blocking PDGFR autophosphorylation with EC50 values of 3.5 nM for PDGFRα Y849 and 5.8 nM for PDGFRβ Y1021. This compound significantly inhibits the proliferation and migration of pulmonary artery smooth muscle cells (PASMCs) by interfering with PDGF-BB-induced ERK1/2 phosphorylation, thus reducing collagen I synthesis and enhancing α-smooth muscle actin expression. WQ-C-401 is a valuable tool for studying mechanisms underlying pulmonary vascular remodeling and holds potential for research in pulmonary arterial hypertension. -
PDGFr Inhibitor
PDGFR-IN-2 is a 4-phenoxyquinoline derivative that acts as a selective inhibitor of the platelet-derived growth factor receptor (PDGFr) with an IC50 value of 0.20 μM. By targeting PDGFr tyrosine kinase activity, PDGFR-IN-2 effectively disrupts downstream signaling pathways associated with cell proliferation and migration. This compound is valuable for research applications investigating the role of PDGFr in various pathological conditions, including cancer and fibrotic diseases. -
PDGFR Inhibitor
DMPQ dihydrochloride is a selective inhibitor of human platelet-derived growth factor receptor β (PDGFRβ), exhibiting an IC50 of 80 nM. This compound demonstrates significant potential in research applications focused on PDGFRβ-mediated signaling pathways, which are implicated in a variety of pathological conditions, including cancer and fibrosis. Its potency and selectivity make DMPQ dihydrochloride a valuable tool for investigating the role of PDGFRβ in cellular processes and therapeutic interventions. -
PDGFR Inhibitor
AG 370 is a selective inhibitor of the platelet-derived growth factor receptor (PDGFR), exhibiting potent activity against PDGF-induced mitogenesis with an IC50 of 20 μM. Additionally, AG 370 demonstrates weak inhibitory effects on the epidermal growth factor receptor (EGFR). This compound is valuable for research applications focused on signaling pathways related to cell proliferation and cancer biology. -
PDGFR-α Inhibitor
PDGFRα kinase-IN-2 is a potent inhibitor of the platelet-derived growth factor receptor alpha (PDGFR-α) with an IC50 of 2.1 nM. This compound exhibits significant anticancer activity against HT-29 human colon cancer cells, with an IC50 of 1.48 μM. Additionally, PDGFRα kinase-IN-2 demonstrates anti-angiogenic properties in zebrafish models while exhibiting low embryonic lethality. It is a valuable tool for research focused on colon cancer and the mechanisms of anti-angiogenesis. -
TGFβRI/PDGFRα Inhibitor
BI-4659 is a dual inhibitor of TGFβRI and PDGFRα, exhibiting IC50 values of 19 nM and 99 nM, respectively. This compound effectively inhibits the kinase activities of both receptors, thereby blocking downstream TGFβRI signaling and reducing Smad2/3 phosphorylation without impacting TGF-β1 expression. BI-4659 is suitable for research applications in pulmonary fibrosis, cancer, and renal ischemia-reperfusion injury studies. -
PDGFRA Inhibitor
GSK190937 is a type II inhibitor of the platelet-derived growth factor receptor alpha (PDGFRA), exhibiting notable antimalarial activity. This compound effectively inhibits hemozoin formation in malaria parasites, leading to the accumulation of free hemoglobin. GSK190937 demonstrates IC50 values of 0.22 μM, 0.59 μM, and 0.25 μM against Plasmodium falciparum strains NF54, K1, and Dd2, respectively. Additionally, it has an IC50 of 25 μM for CHO cells, making it a valuable tool for malaria research. -
PDGFR Inhibitor
KN1022 is a selective inhibitor of the phosphorylation of platelet-derived growth factor receptor (PDGFR), with an IC50 value of 0.24 μM. This compound effectively modulates PDGFR signaling pathways, making it a valuable tool for investigating the role of PDGFR in various cellular processes. It is particularly relevant for research in cancer biology, fibrosis, and other diseases associated with abnormal PDGFR activity. -
PDGFR Inhibitor
Sch 13835 is a selective inhibitor of the platelet-derived growth factor receptor (PDGFR), which plays a critical role in cellular processes such as proliferation, differentiation, and survival. This compound exhibits significant inhibitory activity against PDGFR, making it a valuable tool for studying pathways involved in cancer and fibrosis. Its applications include investigating the role of PDGFR in tumor growth and exploring therapeutic strategies for conditions driven by aberrant PDGFR signaling. -
PDGFR-βInhibitor
Tyrphostin AG1433 hydrochloride is a specific and potent inhibitor of PDGFR-β, with additional activity against KDR/Flk-1. It functions as an angiogenesis inhibitor, making it valuable for research into vascular biology and related pathologies. This compound is suitable for studies focused on cancer, fibrosis, and other diseases where angiogenesis plays a critical role. -
Src Inhibitor
Saracatinib difumarate is a selective Src inhibitor, effectively targeting multiple Src family kinases, including c-Src, Lck, c-YES, Lyn, Fyn, Fgr, and Blk, with IC50 values ranging from 2.7 to 11 nM. This compound demonstrates significant potential in modulating signaling pathways associated with cancer and other diseases driven by Src family kinases. It is commonly utilized in research focusing on cancer biology, cell signaling, and the development of targeted therapies. -
RET/BRAF/S6K/Src Inhibitor
AD57 is an orally active multikinase inhibitor that targets RET, BRAF, S6K, and Src, effectively reducing mTOR activity. This compound demonstrates significant biological activity by interfering with critical signaling pathways involved in cancer proliferation and survival. AD57 is suitable for research applications focused on cancer biology and therapeutic development against malignancies driven by these kinases. -
Src SH2 Inhibitor
pYEEI is a phosphotyrosine-containing tetrapeptide that selectively inhibits the Src SH2 domain with a Kd of 100 nM and an IC50 of 6.5 μM. This compound is pivotal for studying the role of Src signaling pathways in cancer biology and can aid in the development of targeted therapies. Its ability to modulate Src activity makes pYEEI a valuable tool for researchers investigating tumorigenesis and related processes. -
SRC-3 Inhibitor
SRC-3-IN-2 is a selective inhibitor of steroid receptor coactivator 3 (SRC-3), demonstrating potent antitumor activity. This compound is utilized in research focusing on cancer biology and hormone receptor signaling pathways. Its ability to modulate SRC-3 activity makes it a valuable tool for studying SRC-3's role in tumorigenesis and therapeutic resistance. -
Src inhibitor
Fenlean is a natural squamosamide derivative that acts as a Src tyrosine kinase inhibitor. It demonstrates the ability to inhibit over-activated microglia, thereby providing protective effects on dopaminergic neurons. Its anti-inflammatory properties support its potential application in the study and treatment of neuroinflammation in models of Parkinson's disease.
