vegfr in 1

VEGFR inhibitor

VEGFR-3-IN-1 is a novel, potent, and selective VEGFR3 inhibitor with an IC50 of 110.4 nM. It exhibits antitumor activity, inactivates the VEGFR3 signaling pathway, and inhibits the proliferation and migration of VEGF-C-induced human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231, and MDA-MB-436 cells.

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 PDGFR-IN-1 (Compound 1) is an inhibitor of VEGFR with an IC50 of 0.4 μM. It can inhibit angiogenesis in HUVEC cells and holds promise for impeding tumor growth and metastasis.

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 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.

hCA VEGFR-2-IN-1 (compound 13a) is a potent dual inhibitor targeting both Carbonic Anhydrase (CA) IX XII and Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2), exhibiting Ki values of 4.7 nM for hCA XII and 8.3 nM for hCA IX, alongside an IC50 of 26.3 nM for VEGFR-2, and demonstrating anticancer activity [1].

VEGFR PARP-IN-1 (Compound 14b) is a dual inhibitor of VEGFR and PARP with IC50 values of 191 nM and 60.9 nM, respectively. It impairs DNA damage repair pathways, promotes apoptosis, and halts cells in the G2 M phase. This compound demonstrates considerable antiproliferative activity against BRCA wild-type breast cancer cells, with IC50 values of 4.1 μM for MDA-MB-231 cells and 3.5 μM for MCF-7 cells, indicating its potential as an antitumor and anti-metastasis agent [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].

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 AKT-IN-1 (compound 17) is a dual inhibitor of VEGFR-2 and AKT with IC50 values of 0.164 μM and 0.452 μM, respectively. It exhibits antitumor activity.

Famitinib (SHR1020) is a potent orally active multi-targeted kinase inhibitor that effectively inhibits the activity of c-kit, VEGFR-2, and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively [1]. It demonstrates remarkable antitumor properties in human gastric cancer cells and xenografts, inducing apoptosis [2].

Cediranib (AZD2171) (AZD2171) is a highly potent (IC50 < 1 nmol L) ATP-competitive inhibitor of recombinant KDR tyrosine kinase in vitro, also inhibits Flt1 4 (IC50: 5 nM ≤3 nM), similar activity against PDGFRβ and c-Kit, selective more for VEGFR than PDGFR-α (36-fold), CSF-1R (110-fold), and Flt3 (1000-fold) in HUVEC cells.

OSI-930, an orally active inhibitor of c-Kit and the vascular endothelial growth factor receptor-2 (VEGFR-2), targets cancer cell proliferation and blood vessel growth (angiogenesis) in tumors.

JK-P3 is a pyrazole-based inhibitor of VEGFR-2 (IC50: 7.8 μM). JK-P3 inhibits FGFR 1 3 kinase activity in vitro, but has no effect on FGFR signaling in cell-based assays. The compound blocks wound healing and tube formation in HUVEC without effecting endo

Multi-kinase-IN-5 (compound 15c) is a multi-kinase inhibitory agent that demonstrates significant inhibition of a range of protein kinases, including RET (69%), KIT (31%), cMet (62%), VEGFR1 (40%), VEGFR2 (73%), FGFR1 (74%), PDGFR (59%), and BRAF (74%). Its IC50 values are 1.287 μM for FGFR1, 0.117 μM for VEGFR, and 1.185 μM for RET kinases, indicating its potency [1].

Vandetanib Fumarate is an orally available tyrosine kinase inhibitor. Vandetanib Fumarate works by blocking RET (REarranged during Transfection), vascular endothelial growth factor receptor (VEGFR-2, VEGFR-3), and epidermal growth factor receptor and to a

EGFR VEGFR2-IN-1 (Compound 10e) serves as an inhibitor for VEGFR-2 and EGFR, with respective IC50 values of 0.26 and 0.14 μM. It inhibits microtubule protein polymerization with an IC50 of 40.9 μM and induces cell apoptosis (Apoptosis). EGFR VEGFR2-IN-1 is applicable in research related to anti-leukemia and anti-lymphoma treatments.

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.

The Immuno-Oncology Screening Library consists of 2 plates and contains more than 90 cancer and immunology-associated compounds in a 96-well Matrix tube rack format as 10 mM stock solutions in DMSO. This library includes a variety of immuno-oncology target modulators, including but not limited to, adenosine, CCR, CXCR, and TLR agonists and antagonists, BTK, PI3K, VEGFR, and BRAF inhibitors, PD-1/PDL-1 interaction inhibitors, and HDAC inhibitors. Please review the product insert for a full list of targets. Stability data is not available for the compounds as supplied in the screening library.

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].

L-Sepiapterin, also known as Sepiapterin, is a precursor compound crucial for the production of tetrahydrobiopterin (BH4), which serves as a coenzyme for endothelial nitric oxide synthase (eNOS). This compound demonstrates its efficacy by improving endothelial dysfunction in small mesenteric arteries from db db mice and promoting angiogenesis. Moreover, L-Sepiapterin exerts inhibitory effects on cellular proliferation and migration in ovarian cancer cells through the down-regulation of p70S6K-dependent vascular endothelial growth factor receptor-2 (VEGFR-2) expression[1][2].

hVEGF-IN-1 inhibits human VEGF-A translation and has antitumor activity.

Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor that acts on KDR, Flt-1, FGFR1, and PDGFRα with IC50 values of 4 nM, 20 nM, 4 nM, and 2 nM, respectively.