2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. VEGFR
  5. VEGFR1/Flt-1 Isoform

VEGFR1/Flt-1

VEGFR1/Flt-1 is a VEGF receptor tyrosine kinase that binds VEGF-A, VEGF-B, and PlGF, positioning it as a regulator of vascular endothelial growth factor signaling and angiogenesis[1]. Mechanistically, VEGFR1 balances angiogenic output by trapping VEGF-A during embryogenesis while contributing to pathological angiogenesis in adult tissues through macrophage-lineage cell migration and activation[2]. Compared with VEGFR2/KDR, which carries strong tyrosine kinase activity and mediates major endothelial angiogenic signals, VEGFR1 shows weaker kinase activity but higher VEGF-A binding affinity, giving it a distinct modulatory role[3]. VEGFR1 also forms VEGFR1-VEGFR2 heterodimers that support endothelial migration, sustained tube formation, vasorelaxation, and nitric oxide pathway activation without driving proliferation[4]. In disease models, VEGFR1 signaling promotes tumor growth, metastasis, inflammation, and macrophage-associated angiogenesis, while soluble VEGFR1/sFlt-1 acts as an endogenous VEGF inhibitor linked to preeclampsia and proteinuria[5]. For experimental applications, VEGFR1 antagonistic peptides can block VEGF-A, VEGF-B, and PlGF binding, inhibit receptor phosphorylation, reduce endothelial tube formation, and suppress neoangiogenesis without interfering with VEGFR2 activation[6].

References:

Cat. No. Product Name Effect Purity
  • HY-10981
    Lenvatinib
    		Inhibitor 99.75%
    Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
  • HY-50904
    Nintedanib
    		Inhibitor 99.94%
    Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
  • HY-10331
    Regorafenib
    		Inhibitor 99.93%
    Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity.
  • HY-13016
    Cabozantinib
    		Inhibitor 99.97%
    Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis.
  • HY-10065
    Axitinib
    		Inhibitor 99.94%
    Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively.
  • HY-135435
    SU10944
    		Inhibitor
    SU10944 is a selective, orally active VEGFR inhibitor, with an IC50 of 6 nM against VEGFR-1, an IC50 of 96 nM and a Ki of 21 nM against VEGFR-2. SU10944 only exhibits weak inhibitory activity against PDGFRβ (IC50 = 1 μM), SCFR (IC50 = 1.58 μM) and FGFR-1 (IC50 = 1.6 μM). SU10944 selectively inhibits VEGFR receptor downstream signaling, neovascularization, vascular permeability, VEGF-mediated tissue factor production, and induces tumor growth delay. SU10944 can be used in research related to diabetic retinopathy, exudative age-related macular degeneration or cancer.
  • HY-P11649
    NYLTHRQ
    		Inhibitor
    NYLTHRQ is a peptide. NYLTHRQ specifically blocks the interaction between sVEGFR1-i13 and β1 integrin, and inhibits the activation of VEGFR1 and VEGFR2. NYLTHRQ inhibits cancer cell proliferation. NYLTHRQ can be used in the research of tumors such as lung squamous cell carcinoma.
  • HY-182354
    VEGFR2-IN-84
    		Inhibitor
    VEGFR2-IN-84 is an orally active, multi-targeted tyrosine kinase inhibitor based on a naphthalene ring scaffold. VEGFR2-IN-84 inhibits VEGFR2 with sub-nanomolar affinity and broadly targets kinases including Kit, FGFR, PDGFR, and Ret. By competitively binding to the ATP-binding pocket, VEGFR2-IN-84 blocks the phosphorylation of VEGFR2 and its downstream AKT/ERK signaling pathway, thereby significantly inhibiting endothelial cell proliferation, migration, and tumor angiogenesis. VEGFR2-IN-84 exhibits broad-spectrum antiproliferative activity against various solid tumors such as liver cancer, lung cancer, and renal cancer, shows weak toxicity to normal cells, and has superior potency to Lenvatinib (HY-10981). VEGFR2-IN-84 possesses favorable pharmacokinetic properties and high safety (LD50>2000 mg/kg), and can be used in related studies of various malignant tumors.
  • HY-10208
    Pazopanib
    		Inhibitor 99.91%
    Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
  • HY-11106
    Nintedanib esylate
    		Inhibitor 99.96%
    Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
  • HY-10981A
    Lenvatinib mesylate
    		Inhibitor 99.91%
    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.
  • HY-19912
    Fruquintinib
    		Inhibitor 99.98%
    Fruquintinib (HMPL-013) is a highly potent and selective VEGFR 1/2/3 inhibitor with IC50s of 33, 0.35, and 35 nM, respectively.
  • HY-10977
    Tivozanib
    		Inhibitor 99.80%
    Tivozanib (AV-951; KRN951) is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib exhibits antitumor efficacy.
  • HY-50751
    Linifanib
    		Inhibitor 99.39%
    Linifanib (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib shows prominent antitumor activity. Linifanib has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib is a specific miR-10b inhibitor that blocks miR-10b biogenesis.
  • HY-12297
    Sulfatinib
    		Inhibitor 99.52%
    Sulfatinib (Surufatinib) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC50s of in a range of 1 to 24 nM.
  • HY-10338
    Foretinib
    		Inhibitor 99.45%
    Foretinib is a multi-target tyrosine kinase inhibitor with IC50s of 0.4 nM and 0.9 nM for Met and KDR.
  • HY-50905
    Dovitinib
    		Inhibitor 99.88%
    Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity.
  • HY-10205
    Cediranib
    		Inhibitor 99.87%
    Cediranib (AZD2171) is a highly potent, orally available and blood-brain barrier permeability VEGFR tyrosine kinase inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
  • HY-16961
    Sitravatinib
    		Inhibitor 99.57%
    Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively. Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
  • HY-P10284
    S7
    		Inhibitor 98.25%
    S7 is an inhibitory polypeptide targeting IL-6R, which specifically binds to IL-6R and its A chain (gp80/IL-6RA) to block its signal transduction. S7 inhibits IL-6-mediated anti-apoptosis (apoptosis), angiogenesis and the expression of VEGF-A, blocks related survival signaling pathways, and enhances the sensitivity of cancer cells to chemotherapeutic drugs. S7 can be applied to the research of related diseases such as cervical cancer, multiple myeloma, Kaposi's sarcoma, prostate cancer and basal cell carcinoma.
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity