355025-13-7

355025-13-7 structure

Name: Ki16198
Chemical Name: Methyl 3-({4-[4-({[1-(2-chlorophenyl)ethoxy]carbonyl}amino)-3-met hyl-1,2-oxazol-5-yl]benzyl}sulfanyl)propanoate
CAS Number: 355025-13-7
Molecular Formula: C₂₄H₂₅ClN₂O₅S
Molecular Weight: 488.984
Catalog: Biochemical Inhibitor G protein coupled receptor(GPCR & G Protein) LPA Receptor Antagonist
Create Date: 2016-12-30 17:45:51
Modify Date: 2024-01-14 09:13:22
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].

Name	Methyl 3-({4-[4-({[1-(2-chlorophenyl)ethoxy]carbonyl}amino)-3-met hyl-1,2-oxazol-5-yl]benzyl}sulfanyl)propanoate
Synonyms	Methyl 3-({4-[4-({[1-(2-chlorophenyl)ethoxy]carbonyl}amino)-3-methyl-1,2-oxazol-5-yl]benzyl}sulfanyl)propanoate Propanoic acid, 3-[[[4-[4-[[[1-(2-chlorophenyl)ethoxy]carbonyl]amino]-3-methyl-5-isoxazolyl]phenyl]methyl]thio]-, methyl ester Ki16198

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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> GPCR/G Protein >> LPL Receptor
Target	Ki: 0.34 μM (LPA1 receptor) Ki: 0.93 μM (LPA1 receptor)[1]
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].
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.
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.