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Catalog No.
Product Name
Application
Product Information
Citations
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VEGFR-2 inhibitor
Apatinib mesylate(YN968D1 mesylate) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 with an IC50 of 1 nM.
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multi-targeted tyrosine kinase inhibitor
Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities. -
VEGFA inhibitor
PTC299 is a potent, orally bioavailable VEGFA inhibitor, targets dihydroorotate dehydrogenase (DHODH), resulting in cell growth inhibition and differentiation in leukemias, including acute myeloid leukemia, linking DHODH regulation and stress-induced VEGFA and angiogenesis. -
VEGFR/PDGFRβ/KIT inhibitor
N-desethyl sunitinib is a major and pharmacologically active metabolite of sunitinib, which is potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor (Ki values are 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT respectively). -
Tyrosine kinase inhibitor
Regorafenib is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively. -
VEGFR Inhibitor
SU14813 is an oral, multitargeted tyrosine kinase inhibitor (TKI) targeting vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptors (PDGFR), Kit, and fms-like tyrosine kinase 3 (FLT-3). -
VEGFR2/Src kinase inhibitor
TG 100572 is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kinases with IC50 values of 2/7/2/1/0.5 nM for VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse respectively. -
VEGFr2 inhibitor
TG 100801 is the prodrug of TG 100572, TG 100572 is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kinases with IC50 values of 2/7/2/1/0.5 nM or VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse respectively.
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c-Kit/VEGFR2/PDGFRβ inhibitor
Toceranib phosphate is a kinase inhibitor with both antitumor and antiangiogenic activity through inhibition of KIT, vascular endothelial growth factor receptor 2, and PDGFRβ. -
VEGFR/EGFR inhibitor
Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM. -
VEGFR/EGFR Inhibitor
BMS-690514 is a potent and selective inhibitor of epidermal growth factor receptor (EGFR), HER2, and HER4, as well as the VEGF receptor kinases. -
c-Met/VEGFR-2 inhibitor
E7050 (also known as golvatinib is an orally bioavailable dual kinase inhibitor of c-Met (hepatocyte growth factor receptor) and VEGFR-2 (vascular endothelial growth factor receptor-2) tyrosine kinases with potential antineoplastic activity. -
VEGFR1/2/3/PDGFRβ/Kit/RET/Raf-1 inhibitor
Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively. -
multi-targeted receptor tyrosine kinases inhibitor
SU14813 maleate is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT. -
neuropilin-1/VEGF-A inhibitor
EG00229 is the first small molecule inhibitors of the neuropilin-1 and VEGF-A interaction with an IC50 of inhibition of 8 uM(125I-VEGF binding to PAE/NRP1 cells). -
MET/VEGFR-2 inhibitor
BMS-817378 is a novel prodrug of the dual Met/VEGFR-2 inhibitor BMS-794833. -
VEGFR Inhibitor
ZM 323881 is a potent and selective inhibitor of the kinase activity of the human vascular endothelial growth factor receptor 2 (VEGFR2/KDR). -
Raf kinase inhibitor
Sorafenib N-Oxide is a metabolite of Sorafenib, a potent Raf kinase inhibitor. -
c-kit/VEGFR/PDGFR Inhibitor
Famitinib is a potent multi-targeted kinase inhibitor that primarily targets c-kit, VEGFR-2, and PDGFRβ, with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively. This orally active compound demonstrates significant antitumor activity in human gastric cancer cells and xenograft models. Famitinib also induces apoptosis, making it a valuable tool for research in cancer therapeutics and signaling pathways. -
VEGFR2 Inhibitor
JK-P3 is a selective inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) with IC50 values of 7.83 μM for VEGFR2, 27 μM for FGFR1, and 5.18 μM for FGFR3. It effectively blocks VEGF-A-induced VEGFR2 activation and downstream signaling pathways, demonstrating inhibition of endothelial cell migration and angiogenesis in vitro. Additionally, JK-P3 suppresses fibroblast growth factor receptor kinase activity, contributing to its anti-angiogenic properties and making it a valuable tool for research in vascular biology and cancer therapeutics. -
VEGFR/FGFR Inhibitor
Lucitanib dihydrochloride is a selective dual inhibitor targeting VEGFR and FGFR, demonstrating potent inhibition of VEGFR1, VEGFR2, VEGFR3, FGFR1, and FGFR2 with IC50 values of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively. This inhibitor plays a critical role in regulating angiogenesis and tumor growth, making it valuable for research in cancer biology and therapeutic development. Lucitanib dihydrochloride is suitable for studies focused on vascular endothelial growth factor signaling pathways and fibroblast growth factor signaling, contributing to the understanding of tumor microenvironment interactions. -
VEGFR-2/FGF Inhibitor
CP-547632 TFA is a potent, orally active inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2) and Fibroblast Growth Factor (FGF) kinases, exhibiting IC50 values of 11 nM and 9 nM, respectively. This reagent demonstrates notable selectivity for VEGFR-2 and bFGF over other tyrosine kinases, including EGFR and PDGFRβ. CP-547632 TFA is primarily utilized in cancer research due to its antitumor efficacy, making it a valuable tool for studies focused on angiogenesis and tumor development. -
VEGFR-2 And FGFR-1 Inhibitor
BMS-645737 is a selective inhibitor of FGF receptor-1 (FGFR-1) and VEGF receptor-2 (VEGFR-2), acting through competitive inhibition of their tyrosine kinase activity. It exhibits potent anti-angiogenic properties, making it a valuable tool in cancer research and studies related to tumor-induced angiogenesis. Additionally, BMS-645737 has been observed to induce lesions in incisor teeth, further highlighting its potential for studying tissue effects and side effects in therapeutic contexts. -
VEGFR2/MET Inhibitor
Cabozantinib hydrochloride is a potent inhibitor of VEGFR2 and MET, exhibiting IC50 values of 0.035 nM and 1.3 nM, respectively. Additionally, it effectively inhibits other receptor tyrosine kinases including KIT, RET, AXL, TIE2, and FLT3 with IC50 values of 4.6 nM, 5.2 nM, 7 nM, 14.3 nM, and 11.3 nM. This compound demonstrates significant antiangiogenic properties by disrupting tumor vasculature and inducing apoptosis in both tumor and endothelial cells. It is widely utilized in cancer research to explore the mechanisms of tumor progression and treatment resistance. -
c-kit/VEGFR/PDGFR Inhibitor
Famitinib malate is an orally active, multi-targeted kinase inhibitor primarily targeting c-kit, VEGFR-2, and PDGFRβ, with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively. This compound induces cell apoptosis and demonstrates significant anti-tumor activity in human gastric cancer cells and xenograft models. Famitinib malate is a valuable tool for research into cancer therapies and mechanisms of action. -
VEGFR2/KDR Inhibitor
Vatalanib hydrochloride is a potent and selective inhibitor of VEGFR2 (vascular endothelial growth factor receptor 2), with an IC50 of 37 nM. It effectively penetrates the blood-brain barrier, making it suitable for studies involving central nervous system applications. Vatalanib hydrochloride is utilized in research focused on angiogenesis, tumor growth inhibition, and vascular biology, contributing valuable insights into therapeutic strategies for various cancers. -
VEGFR-2 Inhibitor
VEGFR-2-IN-15 is a selective inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2), a key regulator of angiogenesis. This compound effectively arrests cell growth in HepG2 cells at the Pre-G1 phase and induces apoptosis. It is a valuable tool for research applications focused on cancer biology and therapeutic strategies targeting angiogenesis. -
ALK/IR/VEGFR2/TIE2/DLK Inhibitor
CEP-14083 is an ATP-competitive inhibitor targeting ALK, with IC50 values of 2 nM in enzymatic assays. This compound also inhibits other kinases, including the insulin receptor (IR), vascular endothelial growth factor receptor 2 (VEGFR2), angiopoietin-1 receptor (TIE2), and dual leucine zipper kinase (DLK). CEP-14083 has been shown to suppress CD274 mRNA expression and the function of NPM/ALK in NPM/ALK-positive T cell lymphoma cells. It is a valuable tool for research focused on lymphoma and related signaling pathways. -
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.
