Ki16198

Names

[ Name ]:
Ki16198

[Synonym ]:
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

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
594.2±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₄H₂₅ClN₂O₅S

[ Molecular Weight ]:
488.984

[ Flash Point ]:
313.2±30.1 °C

[ Exact Mass ]:
488.117279

[ PSA ]:
119.45000

[ LogP ]:
5.19

[ Vapour Pressure ]:
0.0±1.7 mmHg at 25°C

[ Index of Refraction ]:
1.604

[ Storage condition ]:
-20℃

Related Compounds

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