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Merck
CN

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

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About This Item

Empirical Formula (Hill Notation):
C21H21ClN4O
CAS Number:
729605-21-4
Molecular Weight:
380.87
UNSPSC Code:
12352200
MDL number:
MFCD12828749

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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

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

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).

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

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