vegfr-2

JNJ-38158471 (CS-2660), a highly selective, orally available, well tolerated VEGFR2 inhibitor with IC50 of 40 nM, inhibits closely related tyrosine kinases such as Ret and Kit with IC50 of 180 nM and 500 nM.

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

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.

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

VEGFR-2-IN-38 (compound 3) acts as a potential inhibitor of the vascular endothelial growth factor receptor-2 [1].

VEGFR-2 InhA-IN-1, a dual inhibitor based on pyrazole, targets InhA and VEGFR, exhibiting both anti-tuberculosis and anti-angiogenic properties. It demonstrates effective antibacterial activity against the Mycobacterium tuberculosis H37Rv strain (MIC = 6.25 μg mL) and significantly suppresses VEGFR-2 activity (IC 50 = 15.27 nM).

VEGFR-2-IN-50 (Compound 10f) is a VEGFR-2 inhibitor and apoptosis inducer with an IC50 of 0.33 μM. It exhibits growth inhibitory activity against the MCF-7 and MDA-MB-231 breast cancer cell lines, with IC50 values of 19.86 μM and 10.88 μM, respectively, making it a promising agent for breast cancer research.

VEGFR-2-IN-19 (Compound 15b) is a highly efficacious inhibitor of VEGFR2, a receptor involved in angiogenesis, and induces cellular apoptosis while elevating intracellular reactive oxygen species, making it a promising anticancer agent [1].

TIE-2 VEGFR-2 kinase-IN-4, a benzimidazole derivative, is a potent inhibitor of the tyrosine kinase receptors TIE-2 and VEGFR-2, with IC50 values of 5.2 nM and 5.1 nM, respectively. This compound is utilized in angiogenesis research [1].

VEGFR-2 c-Met-IN-1 is a dual inhibitor of VEGFR-2 and c-Met, with IC50 values of 138 nM and 74 nM, respectively, demonstrating antitumor activity [1].

VEGFR-2 DHFR-IN-2 (compound 5b) is a dual inhibitor targeting VEGFR-2 and DHFR, with respective IC50 values of 0.623 μM and 9.085 μM. It demonstrates potent cytotoxicity against C26, HepG2, and MCF7 cancer cell lines, with IC50 values ranging from 3.59 μM to 8.38 μM. VEGFR-2 DHFR-IN-2 holds promise for cancer research [1].

VEGFR-2 BRAF-IN-1, a dual inhibitor of VEGFR-2 and BRAF kinases, demonstrates potent inhibitory activity with IC50 values of 0.049 µM for VEGFR-2, 0.063 µM for BRAF V600E, and 0.005 µM for BRAF WT. It effectively induces apoptosis and arrests the cell cycle primarily at the G1 S phase.

VEGFR-2-IN-18 (Compound 15d) is a high-potency inhibitor of VEGFR-2, exhibiting an IC50 value of 60 nM. This compound effectively induces cell apoptosis and demonstrates significant antitumor properties [1].

VEGFR-2 DHFR-IN-1 (compound 8b) is a chemical inhibitor of VEGFR-2 and DHFR, with IC50 values of 0.384 μM and 7.881 μM, respectively. It possesses effective antibacterial activity against pathogens including Escherichia coli, Streptococcus faecalis, Salmonella enterica, MSSA, and MRSA, with MIC values ranging from 8 to 16 μg mL. Additionally, it exhibits potent cytotoxicity against cancer cell lines C26, HepG2, and MCF7, with IC50 values between 2.97 and 7.12 μM, making it a valuable tool for cancer research [1].

VEGFR-2-IN-26 (compound 5h) is a potent VEGFR-2 inhibitor (IC50: 15.5 nM) that exhibits significant anti-proliferative effects on leukemia, CNS, non-small lung, ovarian, renal, prostate, and breast cancer cells.

VEGFR-2-IN-27 (compound 7a) is a potent VEGFR-2 inhibitor (IC50: 14.8 nM) suitable for anticancer research.

VEGFR-2-IN-59 (Compound 3h) is an inhibitor of VEGFR2 with an IC50 of 3.73 µM. It exhibits cytotoxicity in cancer cell lines A549, HT-29, A375, MCF7, and NHDF, with IC50 values of 20.91, 19.70, 9.63, 17.43, and 20.71 μM, respectively. VEGFR-2-IN-59 also inhibits tubular structure formation and demonstrates anti-angiogenic properties.

VEGFR-2-IN-64 (Compound 28) is an inhibitor of VEGFR2 with an IC50 of 27.8 nM. It suppresses the proliferation of cancer cells A549, T-47D, and Caco-2, exhibits anti-migration and anti-colony formation activities in T-47D cells, and induces apoptosis in T-47D cells.

VEGFR-2-IN-65 (Compound 07) functions as a VEGFR-2 inhibitor. It forms hydrogen bonds with Cys180 and can inhibit tube formation in HUVECs.

VEGFR-2-IN-52 (compound 14d) serves as a powerful inhibitor of VEGFR-2, exhibiting an IC 50 of 191.1 nM. It effectively reduces the protein expression levels of p-VEGFR-2, MMP9, p-ERK1 2, and p-MEK1. In addition, VEGFR-2-IN-52 demonstrates cytotoxic properties by inducing apoptosis and arresting the cell cycle at the G0 G1 phase, and it enhances the levels of ROS.

VEGFR-2-IN-57 (compound 6n) exhibits significant cytotoxicity on HUVEC cells, with an IC50 value of 28.77 nM.

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].

VEGFR-2-IN-33 (Compound 4d), a potent VEGFR inhibitor with an IC50 value of 61.04 nM, demonstrates significant inhibition of HepG2 cell proliferation with an IC50 of 4.31 nM, and is utilized for hepatocellular carcinoma (HCC) research [1].

VEGFR-2-IN-20 (Compound 7) is a potent VEGFR inhibitor with significant potential for cancer research [1].