XRP44X

XRP44X, is a Ras-Net (Elk-3) pathway inhibitor; tubulin polymerization inhibitor Colchicine binding site.XRP44X is used as an anti-cancer drug targeting epidermal growth factor receptor.

ChEBI: [4-(3-chlorophenyl)-1-piperazinyl]-(5-methyl-2-phenyl-3-pyrazolyl)methanone is a member of piperazines.

A cell-permeable pyrazole compound that is shown to prevent in vitro tubulin polymerization (IC₅₀ = 0.2 μM) by targeting Colchicine (Cat. No. 234115) binding site (Kd = 0.3 μM) in cell-free assays and induce blebs formation in HUVEC cultures by perturbing both tubulin microtubles and actin cytoskeleton structures. Unrelated to its effects on actin and tubulin filaments, XRP44X is also reported to block the activations of Ras and its downstream effector molecules, such as Raf, MEK, Erk, Rsk, and Net (Elk-3/SAP-2/Erp), upon FGF-2 (Cat. No. 341595) stimulation. Potently inhibits the growth of HUVEC, NIH3T3, as well as 9 other cancer cell lines in antiproliferation assays (IC₅₀ ≤11.3 nM).

XRP44X is a Ras-Net (Elk-3) pathway inhibitor; tubulin polymerization inhibitor Colchicine binding site.

Ras: 10 nM (IC₅₀)