Catalog No.
Product Name
Application
Product Information
Citations
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VEGFR2/Tie-2 Inhibitor
TIE-2/VEGFR-2 kinase-IN-2 is a potent dual inhibitor of the Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) and the Tyrosine kinase with immunoglobulin-like and EGF-like domains 2 (Tie-2), exhibiting pIC50 values of 8.61 and 8.56, respectively. This compound serves as an effective anti-angiogenic agent, making it a valuable tool for cancer research. Its ability to inhibit both targets can provide insights into tumor vascularization and growth. -
HIF-1 Inhibitor
Cyclo(CLLFVY) is a selective inhibitor of hypoxia-inducible factor-1 (HIF-1), demonstrating IC50 values of 19 μM in U2OS cells and 16 μM in MCF-7 cells. By binding to the PAS-B domain of HIF-1α, cyclo(CLLFVY) effectively disrupts HIF-1 dimerization and subsequent transcriptional activity. This compound downregulates the expression of key hypoxia response genes, including VEGF and CAIX, and shows potential for antitumor applications in HIF-1 associated cancers. -
VEGFR2 Inhibitor
VEGFR-2-IN-5 hydrochloride is a selective inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2), a critical target involved in angiogenesis and tumor growth. This compound exhibits strong biological activity in inhibiting VEGFR-2 signaling, making it useful for research focused on cancer biology and vascular biology. Its application extends to the study of tumor microenvironments and potential therapeutic strategies targeting angiogenesis in various malignancies. -
VEGFR Inhibitor
Ziv-aflibercept is a soluble vascular endothelial growth factor receptor (VEGFR) inhibitor. It demonstrates significant anti-angiogenic activity by blocking the interaction between VEGF and its receptors, thereby inhibiting endothelial cell proliferation and migration. This compound is primarily investigated for its therapeutic potential in metastatic colorectal carcinoma and various retinal diseases, offering insights into the modulation of tumor growth and ocular pathologies. -
VEGFR2 Inhibitor
Rhamnazin is an orally active inhibitor of VEGFR2 signaling, exhibiting an IC50 of 4.68 μM against VEGFR2 kinase. This compound demonstrates significant antiangiogenic activity and antitumor efficacy, making it a valuable tool in cancer research. Additionally, Rhamnazin possesses antioxidant and anti-inflammatory properties, further broadening its potential applications in biological studies. -
VEGFR Inhibitor
5α-Hydroxycostic acid is a natural eudesmane-type sesquiterpene that functions as a VEGFR inhibitor. It exhibits notable anti-angiogenic properties, effectively inhibiting the migration of breast cancer cells by modulating the VEGF/VEGFR2 and Ang2/Tie2 signaling pathways. This compound is valuable for research applications focused on cancer biology and therapeutic development targeting vascular endothelial growth factor receptors. -
VEGFR2/Tie-2 Inhibitor
GW768505A free base is a potent dual inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) and Tie-2, exhibiting a pIC50 of 7.81 for VEGFR2. This compound demonstrates significant anti-angiogenic activity, making it valuable for research applications in cancer biology and therapeutic angiogenesis. It can be utilized in studies aimed at elucidating the roles of VEGFR2 and Tie-2 in various pathological conditions. -
HIF-2α Inhibitor
Casdatifan is an orally bioavailable allosteric inhibitor targeting hypoxia-inducible factor 2α (HIF-2α). It functions by preventing the heterodimerization of HIF-2α with ARNT, thereby inhibiting pro-tumor gene transcription. Casdatifan has demonstrated significant tumor growth suppression in clear cell renal cell carcinoma (ccRCC) models, both as a single agent and in combination therapies. This reagent is valuable for research related to ccRCC and HIF-2α signaling pathways. -
VEGFR Inhibitor
Bevasiranib sodium is a small interfering RNA (siRNA) targeting the vascular endothelial growth factor receptor (VEGFR). By silencing the genes responsible for VEGF production, it plays a crucial role in the inhibition of choroidal neovascularization (CNV), a significant factor in the development of wet age-related macular degeneration (wet AMD). This reagent is essential for research into therapeutic approaches for retinal diseases and the modulation of angiogenic processes. -
VEGFR-2 Inhibitor
VEGFR-2-IN-37 is a potent inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2). Exhibiting an inhibition rate of approximately 56.9% at 200 μM, this compound demonstrates the potential to hinder the proliferation of human umbilical vein endothelial cells (HUVECs). It is an essential tool for researchers investigating angiogenesis and related vascular processes. -
VEGFR-2 Inhibitor
VEGFR-2-IN-29 is an inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2), demonstrating an IC50 of 16.5 nM. This compound effectively modulates angiogenesis and vascular permeability by inhibiting VEGFR-2 signaling. VEGFR-2-IN-29 is valuable in research related to tumor vasculature, cancer biology, and potential therapeutic interventions for diseases characterized by aberrant angiogenesis. -
VEGFR2 Inhibitor
VEGFR-2-IN-6 is a selective inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR2), an essential target in the modulation of angiogenesis. This compound demonstrates significant biological activity in inhibiting endothelial cell proliferation and tube formation. It is primarily utilized in research concerning cancer therapeutics and other conditions where neovascularization plays a critical role. -
TIE-2/VEGFR-2 Inhibitor
TIE-2/VEGFR-2 kinase-IN-1 is a potent inhibitor targeting the TIE-2 and VEGFR-2 kinases, which are critical regulators of angiogenesis. This compound is instrumental in researching diseases characterized by abnormal blood vessel formation, including various cancers and diabetic retinopathy. Its application facilitates the exploration of therapeutic strategies aimed at modulating angiogenic processes and offers insights into the underlying mechanisms of angiogenesis-related pathologies. -
VEGFR/PDGFR Inhibitor
BMS-605541 is a selective, orally active inhibitor targeting VEGFR-2 kinase, exhibiting an IC50 of 23 nM and a Ki of 49 nM. It also inhibits Flk-1, VEGFR-1, and PDGFR-β with IC50 values of 40 nM, 400 nM, and 200 nM, respectively. This reagent is valuable for cancer research, aiding in the study of angiogenesis and tumor progression. -
VEGFR2 Inhibitor
(Z)-FeCP-oxindole is a selective inhibitor of human vascular endothelial growth factor receptor 2 (VEGFR2), exhibiting an IC50 value of 200 nM. Additionally, it can significantly inhibit VEGFR1 and PDGFRα or β at concentrations of 10 μM. This compound demonstrates notable anticancer activity against B16 murine melanoma cell lines, with an IC50 of less than 1 μM, making it a valuable tool for cancer research and therapeutic studies. -
VEGFR2 Inhibitor
VEGFR2-IN-7 is a selective inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2), a key regulator in angiogenesis. This compound demonstrates potent anticancer activity by interrupting the signaling pathways involved in tumor-associated blood vessel formation. VEGFR2-IN-7 is valuable for research applications targeting tumor vasculature and studying the role of angiogenesis in cancer progression. -
Lck/Src/KDR/VEGF2R/Tie-2/BLK/Csk/Fyn/Lyn Inhibitor
RK-20448 is an ATP-competitive inhibitor targeting Lck, Src, KDR/VEGF2R, and Tie-2, demonstrating IC50 values of 0.24, 1.19, 10.74, and 5.85 µM, respectively. Additionally, it inhibits BLK, Csk, Fyn, and Lyn, with IC50 values of 0.37, 4.27, 2.03, and 0.43 µM, respectively. This compound is valuable for research involving signal transduction pathways mediated by receptor tyrosine kinases and may contribute to studies on cancer and vascular biology. -
VEGFR Inhibitor
Tivozanib hydrate is a selective inhibitor of vascular endothelial growth factor receptors (VEGFR-1, -2, and -3), displaying IC50 values of 30 nM, 6.5 nM, and 15 nM, respectively. This orally active compound demonstrates significant antitumor efficacy, making it a valuable tool for research focused on tumor angiogenesis and vascular biology. Its selectivity and potency facilitate investigations into VEGFR-related pathways and their implications in cancer treatment. -
VEGFR-2 Inhibitor
VEGFR-2-IN-21 is a potent inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2), exhibiting an IC50 of 0.10 μM. This compound demonstrates significant anticancer activity, making it a valuable tool for research in oncology and vascular biology. Its ability to modulate VEGFR-2 signaling can aid in the investigation of tumor growth and metastasis, as well as facilitate the development of targeted therapies. -
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.
