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LCRF-0004

Chemical Structure : LCRF-0004

CAS No.: 1229611-73-7

LCRF-0004 (LCRF0004)

Catalog No.: PC-49516Not For Human Use, Lab Use Only.

LCRF-0004 is a potent and selective RON receptor tyrosine kinase inhibitor with IC50 of 50 nM (ELISA), weakly inhibits c-Met with IC50 of 150 nM and does not inhibit VEGFR2.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

LCRF-0004 is a potent and selective RON receptor tyrosine kinase inhibitor with IC50 of 50 nM (ELISA), weakly inhibits c-Met with IC50 of 150 nM and does not inhibit VEGFR2.
LCRF-0004 potently inhibited RON phosphorylation in cancer cells with IC50 of 30-40 nM, potently inhibited cellular proliferation in the HCT116 lung cancer cells.
LCRF-0004 displayed weak inhibition of c-Met phosphorylation in the MKN-45 gastric carcinoma cell line which over-expresses c-Met, as well as c-Met-dependent cell migration and scattering mediated by HGF.

Physicochemical Properties

M.Wt 578.55
Formula C28H18F4N6O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(3-fluoro-4-((2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl)oxy)phenyl)-1-phenyl-5-(trifluoromethyl)-1H-pyrazole-4-carboxamide

References

1. Raeppel SL, et al. Bioorg Med Chem Lett. 2015 Jun 15;25(12):2527-31.

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