| Description |
Ki16198 is a potent and orally active LPA receptor antagonist, the methyl ester of Ki16425 (HY-13285). Ki16198 inhibits LPA1 and LPA3-induced inositol phosphate production with Ki values of 0.34 μM and 0.93 μM, respectively. Ki16198 is effective for pancreatic cancer tumorigenesis and metastasis in vivo[1].
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| Related Catalog |
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| Target |
Ki: 0.34 μM (LPA1 receptor) Ki: 0.93 μM (LPA1 receptor)[1]
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| In Vitro |
Ki16198 (0-10 μM; 48 hours) is effective to inhibit migration and invasion responses to LPA with a potency similar to that of Ki16425. The inhibitory effects Ki16198 on the invasion response to LPA, but not to EGF in several pancreatic cancer cell lines, including Panc-1,CFPAC-1, and BxPC-3 cells[1]. Ki16198 (10 μM; 48 hours) signifivcantly decreases expression of proMMP-9 protein and mRNA expression in YAPC-PD cells[1].
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| In Vivo |
Ki16198 (oral administaion; 1 mg in 500 ul; 28 days) significantly decreases the degree of metastasis activity in Ki16198-treated mice. Similiar to liver, metastasis to lung and brain in mice is also observed[1]. Animal Model: Male BALB/c nude mice (6 weeks old)[1] Dosage: 1 mg in 500 ul Administration: Oral administaion; 28 days Result: Inhibited lung and liver metastasis in vivo.
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| References |
[1]. Mayumi Komachi, et al. Orally active lysophosphatidic acid receptor antagonist attenuates pancreatic cancer invasion and metastasis in vivo. Cancer Sci. 2012 Jun;103(6):1099-104.
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