[CAS NO. 355025-13-7] Ki16198
PRODUCTS SPECIFICATIONS [355025-13-7]
DESCRIPTION [355025-13-7]
Overview
| MDL | MFCD23704182 |
|---|---|
| Molecular Weight | 488.98 |
| Molecular Formula | C24H25ClN2O5S |
| SMILES | O=C(OC)CCSCC1=CC=C(C2=C(NC(OC(C3=CC=CC=C3Cl)C)=O)C(C)=NO2)C=C1 |
Summary
Ki16198 is a potent and orally active LPA receptor antagonist, the methyl ester of Ki16425 (HY-13285). Ki16198 inhibits LPA 1 and LPA 3 -induced inositol phosphate production with K i values of 0.34 μM and 0.93 μM, respectively. Ki16198 is effective for pancreatic cancer tumorigenesis and metastasis in vivo [1] .
IC50 & 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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 204.51 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.0451 mL | 10.2254 mL | 20.4507 mL |
| 5 mM | 0.4090 mL | 2.0451 mL | 4.0901 mL |
| 10 mM | 0.2045 mL | 1.0225 mL | 2.0451 mL |