340267-36-9
340267-36-9 structure
- Name: CAY10404
- Chemical Name: 3-(4-methylsulfonylphenyl)-4-phenyl-5-(trifluoromethyl)-1,2-oxazole
- CAS Number: 340267-36-9
- Molecular Formula: C17H12F3NO3S
- Molecular Weight: 367.342
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2016-09-29 06:35:24
- Modify Date: 2024-10-01 16:44:23
-
CAY10404 is a potent and highly selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM. CAY10404 exhibits no inhibition of COX-1 (IC50>500 µM)[1]. CAY10404 is a potent inhibitor of PKB/Akt and MAPK signaling pathways and induces apoptosis in NSCLC cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities[2][3].
| Name | 3-(4-methylsulfonylphenyl)-4-phenyl-5-(trifluoromethyl)-1,2-oxazole |
|---|---|
| Synonyms |
3-[4-(Methylsulfonyl)phenyl]-4-phenyl-5-(trifluoromethyl)-1,2-oxazole
Isoxazole, 3-[4-(methylsulfonyl)phenyl]-4-phenyl-5-(trifluoromethyl)- |
| Description | CAY10404 is a potent and highly selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM. CAY10404 exhibits no inhibition of COX-1 (IC50>500 µM)[1]. CAY10404 is a potent inhibitor of PKB/Akt and MAPK signaling pathways and induces apoptosis in NSCLC cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities[2][3]. |
|---|---|
| Related Catalog | |
| Target |
COX-2:1 nM (IC50) COX-1:>500 μM (IC50) Akt |
| In Vitro | CAY10404 is a potent and selective COX-2 inhibitor with a selectivity index (SI; COX-1 IC50/COX-2 IC50) of >500000[1]. CAY10404 (10-100 µM; for 3 days) inhibits the growth of NSCLC cell lines in a concentration-dependent manner and has an average 50% inhibitory concentration (IC50) of 60-100 µM[3]. CAY10404 (20-100 µM; for 3 days) induces apoptosis in NSCLC cells[3]. CAY10404 (80 µM; for 3 days) induces a concentration-dependent decrease in the level of the anti-apoptotic proteins (Bcl-2 and Bcl-XL) and pAkt and pGSK-3β[3]. CAY10404 (20, 50, 80, 100 µM; for 14 days) compromises the ability of H460 cells to form colonies in anchorage-independent growth in a concentration-dependent manner[3]. Cell Viability Assay[3] Cell Line: Non-small cell lung cancer (NSCLC) cells (H-1703, H-358, H-460) Concentration: 10-100 µM Incubation Time: For 3 days Result: Inhibited the growth of NSCLC cell lines in a concentration-dependent manner. Apoptosis Analysis[3] Cell Line: H460 cells Concentration: 20, 50, 100 µM Incubation Time: For 3 days Result: Induced apoptosis in NSCLC cells. Western Blot Analysis[3] Cell Line: NSCLC cells (H-358, H-460) Concentration: 80 µM Incubation Time: For 3 days Result: Induced a concentration-dependent decrease in the level of the anti-apoptotic proteins (Bcl-2 and Bcl-XL) and pAkt and pGSK-3β, without changing the level of the pro-apoptotic protein (Bax) and total Akt and GSK-3β protein levels. |
| In Vivo | CAY10404 (50 mg/kg/day; ip; for 4 days) decreases lung inflammation in HTV mice and attenuates ventilator-induced lung injury[2]. Animal Model: Adult male C57Bl/6J mice weighing 24-30 g[2] Dosage: 50 mg/kg Administration: IP; daily; for 4 days Result: Attenuated cyclooxygenase activity, significantly decreasing BAL PGE2 and 6-keto PGF1α. Decreased lung inflammation in HTV mice (high tidal volume; 20 ml/kg; for 4 hours) and attenuates ventilator-induced lung injury. |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 498.6±45.0 °C at 760 mmHg |
| Melting Point | 196.47 °C(Predicted) |
| Molecular Formula | C17H12F3NO3S |
| Molecular Weight | 367.342 |
| Flash Point | 255.3±28.7 °C |
| Exact Mass | 367.049011 |
| PSA | 68.55000 |
| LogP | 2.92 |
| Vapour Pressure | 0.0±1.2 mmHg at 25°C |
| Index of Refraction | 1.538 |
| Hazard Codes | Xi |
|---|