ARQ-197 Inhibitor CAS No. 905854-02-6

Cat. No.	Name	Size	Price
KI2814	ARQ-197	5 mg	$110
	ARQ-197	10 mg	$176
	ARQ-197	20 mg	$282
	ARQ-197	50 mg	$752
	ARQ-197	100 mg	$1204
	ARQ-197	200 mg	$2032
	ARQ-197	1 g	$3250

Chemical Characteristic

Product Name	ARQ-197
Synonyms	Tivantinib
CAS No.	905854-02-6
Molecular Weight	369.4
Formula	C₂₃H₁₉N₃O₂
Chemical Name	(3R,4R)-3-(2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinolin-6-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione
Smiles	N1C(=O)[C@H]([C@@H](C1=O)c1c[nH]c2c1cccc2)c1c2cccc3CCCn(c23)c1
Chemical Structure

Biological activities

ARQ-197 is the first non-ATP-competitive and selective c-Met receptor inhibitor. ARQ 197 inhibits human recombinant c-Met with a Ki of about 355 nM. In vitro, ARQ 197 treatment 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 an IC50 ranging from 100 to 300 nM. In vitro cytotoxicity assay, ARQ 197 exerts significant antiproliferative effects in cancer cell lines (including MDA-MB-231, NCI-H441, A549, and SK-OV-3) harboring c-Met and expressing phospho-c-Met to varying degrees with IC50s ranging from 300 to 660 nM. However, in the human cell lines (including SK-MEL-28, NCI-H661, and NCI-H446) with no immunodetectable c-Met or phospho-c-Met, ARQ 197 treatment has little antiproliferative effect. ARQ 197 also increases caspase-dependent apoptosis in c-Met-expressing human cancer cells in vitro. In xenograft mouse models using HT29, MKN-45, and MDA-MB-231 human cancer cell lines, ARQ 197 administration ( 200 mg/kg) significantly inhibits tumor growth and has no significant body weight changes.^[1] In a mouse model of human breast cancer in vivo, ARQ 197 has dose-dependent antimetastatic activity. Moreover, ARQ 197 at 120 mg/kg dose reduces subcutaneous tumor growth, and induces significant inhibition of metastatic growth of breast cancer cells in bone and a noteworthy reduction of tumor-induced osteolysis.^[2]

Protocols

In vitro, ARQ 197 is dissolved in DMSO.^[3]

References

[1] Munshi N, et al. ARQ 197, a novel and selective inhibitor of the human c-Met receptor tyrosine kinase with antitumor activity. Mol Cancer Ther. 2010, 9(6): 1544-1553. [2] Previdi S, et al. Breast cancer-derived bone metastasis can be effectively reduced through specific c-MET inhibitor tivantinib (ARQ 197) and shRNA c-MET knockdown. Mol Cancer Ther. 2012, 11(1): 214-223. [3] Katayama R, et al. Cytotoxic activity of tivantinib (ARQ 197) is not due solely to c-MET inhibition. Cancer Res. 2013, 73(10): 3087-3096.

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