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VEGFR-2 Inhibitor
VS 8 is a potent oral inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2), exhibiting significant anti-angiogenic properties. This compound promotes apoptosis in cancer cells and inhibits cellular migration, making it relevant for studies targeting tumor progression. Additionally, VS 8 demonstrates activity against cancer stem cells (CSCs), providing insights for research in cancer treatment and therapeutic resistance. -
Tubulin/VEGFR Inhibitor
Tubulin/VEGFR-2-IN-2 is an orally active inhibitor targeting tubulin and VEGFR-2, exhibiting IC50 values of 3.27 μM and 0.09 μM, respectively. This compound demonstrates significant antitumor activity by enhancing reactive oxygen species generation, disrupting mitochondrial membrane potential, inducing apoptosis, and arresting the cell cycle. Additionally, Tubulin/VEGFR-2-IN-2 possesses anti-angiogenic effects, impairing endothelial cell migration, invasion, and tube formation in vitro. It effectively suppresses angiogenesis, tumor growth, and metastasis in vivo, making it a valuable tool for research involving non-small cell lung cancer, breast cancer, gastric cancer, and lymphoma. -
VEGFR-2 Inhibitor
VEGFR-2-IN-52 is a potent inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2), demonstrating an IC50 of 191.1 nM. This compound effectively downregulates the expression of phosphorylated VEGFR-2, MMP9, and key signaling proteins p-ERK1/2 and p-MEK1. In addition to its cytotoxic effects, VEGFR-2-IN-52 induces apoptosis and promotes cell cycle arrest in the G0/G1 phase. Furthermore, it enhances reactive oxygen species (ROS) levels, making it valuable for research in cancer therapeutics and angiogenesis studies. -
VEGFR/PARP Inhibitor
VEGFR/PARP-IN-1 is a dual inhibitor targeting Vascular Endothelial Growth Factor Receptor (VEGFR) and Poly(ADP-ribose) Polymerase (PARP), with IC50 values of 191 nM and 60.9 nM, respectively. This compound inhibits DNA damage repair mechanisms, induces apoptosis, and causes G2/M phase cell cycle arrest. It demonstrates significant antiproliferative activity against BRCA wild-type breast cancer cell lines, specifically MDA-MB-231 and MCF-7, with IC50 values of 4.1 μM and 3.5 μM, respectively. VEGFR/PARP-IN-1 is an effective antitumor and anti-metastatic agent, making it valuable for cancer research applications. -
VEGFR-2/HDAC Dual Inhibitor
VEGFR2/HDAC1-IN-1 is a potent dual inhibitor of VEGFR-2 and HDAC, demonstrating IC50 values of 57.83 nM and 9.82 nM, respectively. This compound effectively arrests the cell cycle at the S and G2 phases, leading to apoptosis in HeLa cells. Additionally, VEGFR2/HDAC1-IN-1 exhibits significant anti-angiogenic properties, making it a valuable tool for research in cancer biology and targeted therapies. -
VEGFR Inhibitor
VEGFR-IN-3 is a selective VEGFR inhibitor that demonstrates significant antiproliferative activity against OVCAR-4 and MDA-MB-468 cancer cell lines, with IC50 values of 0.29 μM and 0.35 μM, respectively. This compound is valuable for research applications focused on cancer biology, particularly in studies investigating angiogenesis and tumor growth modulation. Its efficacy makes it a suitable candidate for exploring therapeutic strategies targeting vascular endothelial growth factor receptor pathways. -
PI3K/VEGFR2 Inhibitor
PI3K/VEGFR2-IN-1 is a highly effective dual inhibitor of PI3K and VEGFR2, exhibiting IC50 values of 2.21 μM and 68 μM, respectively. This compound has been shown to induce apoptosis in various cancer cell lines. It is suitable for research applications focused on cancer biology and therapy development targeting the PI3K/VEGFR2 signaling pathways. -
VEGFR2 Inhibitor
YLL545 is a potent inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2), effectively blocking VEGF-induced phosphorylation of VEGFR2 and preventing the activation of downstream signaling mediators such as phosphorylated STAT3 and phosphorylated ERK1/2 in human umbilical vein endothelial cells (HUVEC). This compound demonstrates significant anti-angiogenic properties by suppressing the proliferation, migration, and invasion of HUVEC. Furthermore, YLL545 has shown the capability to induce apoptosis in breast cancer models and inhibit tumor growth, making it a valuable tool for cancer research and the study of angiogenesis. -
VEGFR2 Inhibitor
VEGFR-2-IN-18 is a potent inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2) with an IC50 of 60 nM. This compound induces apoptosis in targeted cells and exhibits significant antitumor activity. It is a valuable reagent for research applications focused on angiogenesis, cancer biology, and the development of targeted therapies. -
VEGFR-2 Inhibitor
VEGFR-2-IN-23 is a highly selective inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2), exhibiting an IC50 value of 0.34 nM. This compound demonstrates significant antitumor activity by inducing apoptosis and causing cell cycle arrest at the G1 phase. VEGFR-2-IN-23 is particularly relevant for research focused on oncology and angiogenesis, providing valuable insights into therapeutic strategies targeting vascular growth pathways. -
VEGFR2 Inhibitor
VEGFR-2-IN-19 is a potent inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2). This compound has been shown to induce apoptosis in cancer cells and elevate intracellular levels of reactive oxygen species. VEGFR-2-IN-19 is primarily utilized in cancer research, offering potential therapeutic insights into tumor progression and vascularization. -
VEGFR-2 Inhibitor
VEGFR-2-IN-13 is a potent inhibitor of the vascular endothelial growth factor receptor-2 (VEGFR-2), demonstrating an IC50 value of 3.4 nM. This compound effectively disrupts the cell cycle in HepG2 cells by inducing G2/M phase arrest and triggering apoptosis. VEGFR-2-IN-13 is valuable for research applications focusing on angiogenesis, cancer development, and therapeutic interventions targeting tumor growth. -
VEGFR-2 Inhibitor
VEGFR-2-IN-28 is a selective inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2) with an IC50 value of 0.83 µM. This compound has been shown to induce apoptosis in cancer cells, highlighting its potential as an anticancer agent. VEGFR-2-IN-28 is suitable for research applications focused on tumor vascularization and the mechanisms of cancer cell survival signaling. -
VEGFR-2/β-tubulin Inhibitor
VEGFR-2-IN-22 is a dual inhibitor targeting VEGFR-2 and β-tubulin polymerization, demonstrating an IC50 of 19.82 nM against VEGFR-2. This compound promotes apoptosis, making it a valuable tool for studying angiogenesis and cancer biology. Its mechanism of action provides insights into vascular endothelial growth factor pathways and their role in tumor progression. -
EGFR/VEGFR2 Inhibitor
EGFR/VEGFR2-IN-3 is a selective inhibitor of the epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor 2 (VEGFR-2), demonstrating IC50 values of 0.129 µM and 0.142 µM, respectively. This compound also exhibits activity against cyclooxygenase-2 (COX-2) with an IC50 of 3.428 µM. EGFR/VEGFR2-IN-3 has been shown to induce cytotoxic effects, promoting apoptosis and causing cell cycle arrest at the G2/M phase. Its dual inhibition profile makes it a valuable tool for research in cancer biology and therapeutic development. -
VEGFR Inhibitor
Aflibercept (VEGF Trap) acts as a soluble decoy receptor targeting vascular endothelial growth factor (VEGF) and inhibiting VEGF receptor (VEGFR) signaling. By fusing the immunoglobulin domains of VEGFR1 and VEGFR2 with the Fc region of human IgG1, Aflibercept effectively diminishes VEGF-mediated biological processes. This reagent is primarily utilized in research related to age-related macular degeneration (AMD) and cardiovascular disease, facilitating studies on angiogenesis and vascular permeability. -
VEGFR inhibitor
Tivozanib hydrochloride hydrate is a selective inhibitor targeting vascular endothelial growth factor receptors (VEGFR)-1, 2, and 3, with 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 cancer research. Tivozanib hydrochloride hydrate is primarily utilized in studies focusing on angiogenesis and tumor proliferation, contributing to the advancement of targeted cancer therapies. -
VEGFR1 Antagonist
GNQWFI is a VEGFR1-specific antagonist that effectively disrupts the interaction between VEGFR1 and its ligands, including VEGFA, VEGFB, and placental growth factor (PlGF). This peptide inhibits VEGF-mediated endothelial cell migration and tube formation, making it a valuable tool for studying vasculature-related processes. GNQWFI has potential applications in cancer research, asthma, and various ocular diseases. -
VEGFR Inhibitor
AAL993 is a potent inhibitor of Vascular Endothelial Growth Factor Receptors (VEGFR) with IC50 values of 130 nM for VEGFR1, 23 nM for VEGFR2, and 18 nM for VEGFR3. This compound selectively targets VEGFRs while showing reduced inhibition of other tyrosine kinases. AAL993 exhibits significant antiangiogenic and antitumor activities, making it a valuable tool for cancer research and studies focused on tumor vasculature modulation. -
VEGFR3 inhibitor
VEGFR-3-IN-1 is a selective inhibitor of Vascular Endothelial Growth Factor Receptor 3 (VEGFR3) with an IC50 of 110.4 nM. It effectively inhibits the proliferation and migration of human dermal lymphatic endothelial cells (HDLEC), as well as breast cancer cell lines MDA-MB-231 and MDA-MB-436, by disrupting the VEGFR3 signaling pathway. This compound demonstrates significant potential in breast cancer research and therapies targeting lymphatic endothelial function. -
VEGFR Inhibitor
DMH4 is a selective inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2), demonstrating potent activity with an IC50 of 0.16 µM. This reagent is valuable for research applications targeting angiogenesis and tumor growth, allowing for the investigation of cancer biology and potential therapeutic interventions. -
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. -
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. -
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. -
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. -
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.

