480150-M

Ras-Net (Elk-3) Pathway Inhibitor, XRP44X

The Ras-Net (Elk-3) Pathway Inhibitor, XRP44X, also referenced under CAS 729605-21-4, controls the biological activity of Ras-Net (Elk-3).

• Synonym(s): Ras-Net (Elk-3) Pathway Inhibitor, XRP44X, Actin Assembly Inhibitor XVI, Ras Activation Inhibitor, Tubulin Polymerization Inhibitor IX, 1-(3-Chlorophenyl)-4-((3-methyl-1-phenyl-1H-pyrazol-5-yl)carbonyl)piperazine
• Empirical Formula (Hill Notation): C₂₁H₂₁ClN₄O
• CAS Number: 729605-21-4
• Molecular Weight: 380.87
• MDL number: MFCD12828749
• UNSPSC Code: 12352200

Properties

• assay: ≥98% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 100 mM; ethanol: 50 mM
• storage temp.: 2-8°C
• InChI: 1S/C21H21ClN4O/c1-16-14-20(26(23-16)18-7-3-2-4-8-18)21(27)25-12-10-24(11-13-25)19-9-5-6-17(22)15-19/h2-9,14-15H,10-13H2,1H3
• InChI key: NPHPNBGYPKBDDB-UHFFFAOYSA-N

Description

General description

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).

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Wasylyk, C., et al. 2008. Cancer Res.68, 1275.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3