p-vegfr2

XL092 (JUN04542) is an Axl Mer cMet KDR inhibitor for the treatment of Axl and Mer receptor tyrosine kinase- dependent disorders.

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

FLT3-IN-37 (Compound 6z) is a potent inhibitor of FLT3-ITD, with IC50 values of 1.5 nM for FLT3-ITD and 3.4 nM for TEL-VEGFR2. It exhibits high selectivity for FLT3 wild-type (WT) and c-Kit. The compound inhibits FLT3 phosphorylation and downregulates the expression of p-Akt, p-STAT5, and p-ERK. By causing cell cycle arrest and inducing apoptosis, FLT3-IN-37 demonstrates anti-leukemic activity, making it suitable for research into acute myeloid leukemia (AML).

Azurin (50-77) is a peptide fragment derived from the copper-containing bacterial protein azurin, present in P. aeruginosa. It exhibits properties that regulate the cell cycle, inhibit cancer proliferation, and manage angiogenesis, proving its potential as an anticancer agent. Specifically, this compound acts as a VEGFR2 inhibitor with an IC20 of approximately 10.7 µM. At a concentration of 20 µM, it effectively induces cell cycle arrest at the G2/M phase in MCF-7 breast cancer cells, while a higher concentration of 50 µM significantly reduces the proliferation of both MCF-7 and ZR-75-1 breast cancer cell lines. Furthermore, Azurin (50-77) impedes VEGF-A-induced capillary tube formation with an IC50 of 12 µM, and alters the cellular and extracellular levels of critical signaling and structural proteins such as F-actin, focal adhesion kinase (FAK), paxillin, and platelet endothelial cell adhesion molecule-1 (PECAM-1) in human umbilical vein endothelial cells (HUVECs) at a concentration of 25 µM. Demonstrating its efficacy in vivo, Azurin (50-77) administered at 10 mg/kg per day notably reduces tumor volume in an MCF-7 mouse xenograft model, highlighting its therapeutic potential.