Ki16198( —— )

Catalog No. M19446 CAS No. 355025-13-7

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Product Name

Ki16198
Note

Research use only, not for human use.
Brief Description

Ki16198 is the methyl ester of Ki16425 which is a LPA antagonist and inhibits LPA1- and LPA3-induced inositol phosphate production with Ki of 0.34 μM and 0.93 μM.
Description

Ki16198 is the methyl ester of Ki16425 which is a LPA antagonist and inhibits LPA1- and LPA3-induced inositol phosphate production with Ki of 0.34 μM and 0.93 μM respectively shows weaker inhibition for LPA2 no activity at LPA4 LPA5 LPA6.
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.Ki16198 (10 μM; 48 hours) signifivcantly decreases expression of proMMP-9 protein and mRNA expression in YAPC-PD cells.
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. Animal Model:Male BALB/c nude mice (6 weeks old) Dosage:1 mg in 500 ul Administration:Oral administaion; 28 days Result:Inhibited lung and liver metastasis in vivo.
Synonyms

——
Pathway

GPCR/G Protein
Target

LPA Receptor
Recptor

LPA1 LPA3
Research Area

Cancer
Indication

Cancer

CAS Number

355025-13-7
Formula Weight

488.98
Molecular Formula

C24H25ClN2O5S
Purity

>98% (HPLC)
Solubility

DMSO:89 mg/mL (182 mM);Ethanol:33 mg/mL (67.5 mM);Water:<1 mg/mL
SMILES

COC(=O)CCSCC1=CC=C(C=C1)C1=C(NC(=O)OC(C)C2=C(Cl)C=CC=C2)C(C)=NO1
Chemical Name

3-(4-(4-((1-(2-Chlorophenyl)ethoxy)carbonylamino)-3-methyl-5-isoxazolyl)benzylsulfanyl)propanoic acid methyl ester

1.Komachi M et al. Cancer Sci 2012 103(6) 1099-1104.

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