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Tivantinib

Chemical Structure : Tivantinib

CAS No.: 905854-02-6

Tivantinib (ARQ-197, ARQ197)

Catalog No.: PC-45842Not For Human Use, Lab Use Only.

Tivantinib (ARQ-197) is a potent, selective, non-ATP-competitive inhibitor of c-Met with Ki of 355 nM.

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Biological Activity

Tivantinib (ARQ-197) is a potent, selective, non-ATP-competitive inhibitor of c-Met with Ki of 355 nM.
Tivantinib (ARQ-197) has no inhibition for EGFR, InsR, PDGFRα, FGFR1 and FGFR4 etc., only modest inhibition (35%) for Ron at 30 uM.
Tivantinib (ARQ-197) inhibits constitutive c-Met phosphorylation in HT29 and MKN-45 cells, and HGF-induced c-Met phosphorylation in MDA-MB-231 and NCI-H441 cells with IC50 of 100-300 nM.
Tivantinib (ARQ-197) shows antiproliferative activity against multiple cancer cell lines (IC50=0.03-30 uM).
Tivantinib (ARQ-197) exerts tumor growth inhibition in multiple mouse xenograft; orally active.

Physicochemical Properties

M.Wt 369.4159
Formula C23H19N3O2
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

2,5-Pyrrolidinedione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-, (3R,4R)-

References

1. Munshi N, et al. Mol Cancer Ther. 2010 Jun;9(6):1544-53.

2. Eathiraj S, et al. J Biol Chem. 2011 Jun 10;286(23):20666-76.

3. Previdi S, et al. Mol Cancer Ther. 2012 Jan;11(1):214-23.

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