vegfr 2

TIE-2/VEGFR-2 kinase-IN-5 (TIE-2 and VEGFR-2 tyrosine kinase receptor inhibitor) is a potent agent with anti-angiogenic activity, commonly used in biomedical research focused on angiogenesis.

VEGFR2-IN-1 is a selective and potent VEGFR2 inhibitor with antitumor activity that inhibits cell proliferation and migration and can be used in the study of breast cancer.

VEGFR-2-IN-6 (WO 02/059110, example 64) is a potent inhibitor of VEGFR2, a crucial receptor involved in the regulation of angiogenesis [1].

VEGFR-2-IN-29 is a VEGFR2 inhibitor.

SU5408 (VEGFR2 Kinase Inhibitor I) is a potent, cell-permeable inhibitor of the VEGFR2 kinase.

VEGFR-2-IN-9 (KDR-in-4) is a potent KDR/VEGFR2 inhibitor with an IC50 of 7 nM, suitable for breast cancer research.

EGFR/VEGFR2-IN-4 (Compound 19) is an irreversible inhibitor of both EGFR and VEGFR-2, exhibiting IC50 values of 18.7 nM and 102.3 nM, respectively, under conditions of 1 μM ATP.

EGFR/VEGFR2-IN-9 (Compound 9b) is an inhibitor of VEGFR-2 (IC50 = 1.325 μM) and EGFR (IC50 = 1.891 μM). It significantly suppresses the proliferation of various cancer cell lines, particularly leukemia cells. EGFR/VEGFR2-IN-9 increases the expression levels of Bax, caspase-3, and p53, while decreasing Bcl-2 expression. This compound induces apoptosis and causes cell cycle arrest at the G1 phase. It is suitable for research on anti-tumor angiogenesis and multidrug-resistant cancers.

Vascular endothelial growth factor receptor 2 (VEGFR2, also known as KDR and FLK1) is a receptor tyrosine kinase that regulates angiogenesis, vascular development, and embryonic hematopoiesis in response to VEGF isoforms A, C, and D. VEGFR2 kinase inhibitor II is a reversible, cell-permeable inhibitor of VEGFR2's kinase activity (IC50 = 70 nM). It less potently inhibits the platelet-derived growth factor receptor β (PDGFRβ; IC50 = 920 nM) and related receptor and non-receptor tyrosine kinases. VEGFR2 kinase inhibitor II blocks the growth of human umbilical vein endothelial cells stimulated with either VEGF or PDGF (IC50s = 110 nM and 2 μM, respectively).

VEGFR2/HDAC1-IN-1 (compound 13) is a potent dual inhibitor of VEGFR-2 and HDAC, with IC50 values of 57.83 nM for VEGFR-2 and 9.82 nM for HDAC. It arrests the cell cycle at the S and G2 phases and induces apoptosis in HeLa cells, demonstrating an anti-angiogenic effect [1].

TIE-2/VEGFR-2 kinase-IN-1 is employed in the synthesis of TIE-2 and/or VEGFR-2 inhibitors for studying diseases associated with inappropriate angiogenesis [1].

VEGFR2-IN-2 has anti-inflammatory and analgesic activities.

FLT3/VEGFR2-IN-1 (Compound 26) is a potent inhibitor of FLT3, VEGFR2, and HDAC, exhibiting IC50 values of 14.5 nM, 3.9 nM, and 30.8 nM against FLT3, VEGFR2, and HDAC1, respectively. It effectively inhibits the phosphorylation of STAT3 and ERK1/2, as well as the proliferation of leukemia cells. FLT3/VEGFR2-IN-1 demonstrates antitumor activity and is applicable in research on acute myeloid leukemia.

EGFR/VEGFR2-IN-5 (Compound 14) is an orally active dual inhibitor of EGFR and VEGFR2, exhibiting an IC50 value of 1.15 µM for VEGFR2 and 0.28 µM for EGFRT790M. This compound demonstrates significant anticancer activity.

EGFR/VEGFR2-IN-6 (Compound 3k) is a dual inhibitor targeting EGFR and VEGFR2, exhibiting IC50 values of 10.53 μM for EGFR and 3.37 μM for VEGFR2. It demonstrates significant antiproliferative activity against breast cancer cells and induces G0/G1 cell cycle arrest and apoptosis, particularly early apoptosis. EGFR/VEGFR2-IN-6 is applicable in cancer research.

EGFR/VEGFR2-IN-10 is a selective inhibitor of EGFR, VEGFR2, and COX2 with IC50 values of 8.5, 68, and 158 nM, respectively. This compound can induce G1 phase cell cycle arrest in MCF-7 cells. EGFR/VEGFR2-IN-10 increases the Bax/Bcl-2 ratio, upregulates caspase-8 expression, and elevates caspase-9 protein levels, thereby activating the intrinsic apoptotic pathway. It demonstrates favorable selectivity by inhibiting tumor proliferation, angiogenesis, and inflammation pathways. EGFR/VEGFR2-IN-10 serves as a tool for the study of cervical cancer, liver cancer, colon cancer, and breast cancer.

PI3K/VEGFR2-IN-1 is a potent dual inhibitor targeting PI3K (IC50: 2.21 μM) and VEGFR2 (IC50: 68 μM), which induces apoptosis and is utilized in cancer research [1].

VEGFR2-IN-4 (compound 25) is a potent and selective VEGFR2 kinase inhibitor with a GI50 of 0.7 nM and demonstrates anti-angiogenic properties, utilized in rheumatoid arthritis research [1].

FGFR1/VEGFR2-IN-1 (compound 2b) is a dual inhibitor of FGFR1 and VEGFR2, utilized in cancer research [1].

VEGFR2-IN-3 (compound 385) is a potent VEGFR2 inhibitor [1].

Anti-VEGFR2/KDR/CD309 Antibody (AT001) is a human antibody expressed in CHO cells, specifically targeting VEGFR2/KDR/CD309. It features a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 145 kDa. For an isotype control, refer to HumanIgG4kappa, Isotype Control.

Anti-VEGFR2/KDR/CD309 Antibody is a human-derived antibody expressed in CHO cells, targeting VEGFR2/KDR/CD309. This antibody features a muIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 150 kDa. For its isotype control, refer to HumanIgG1kappa, Isotype Control.

Axitinib (AG-013736) is a multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1, VEGFR2, VEGFR3, and PDGFRβ (IC50=4/20/0.4/2 nM). Axitinib has antitumor activity and is used in the treatment of renal cell carcinoma.

Nintedanib (Intedanib) is a triple vascular kinase inhibitor that inhibits VEGFR1, VEGFR2, and VEGFR3 (IC50=34/13/13 nM), FGFR1, FGFR2, and FGFR3 (IC50=69/37/108 nM), PDGFRα, and PDGFRβ (IC50=59/65 nM). Nintedanib has antitumor activity and inhibits tumor growth by inhibiting angiogenesis.