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  3. CAY10404

CAY10404 

目录号: HY-121537 纯度: >99.0%
产品使用指南

CAY10404 是一种有效且高度选择性的环氧合酶 2 (COX-2) 抑制剂,IC50 为 1 nM。CAY10404 对 COX-1 没有抑制作用 (IC50>500 µM)。CAY10404 是有效的 PKB/AktMAPK 信号通路抑制剂,可诱导 NSCLC 细胞凋亡 (apoptosis)。CAY10404 是一种二芳基异恶唑,具有良好的止痛,抗炎和抗癌活性。

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CAY10404 Chemical Structure

CAY10404 Chemical Structure

CAS No. : 340267-36-9

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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].

IC50 & Target[1]

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.
Molecular Weight

367.34

Formula

C₁₇H₁₂F₃NO₃S

CAS No.

340267-36-9

SMILES

FC(C1=C(C2=CC=CC=C2)C(C3=CC=C(S(=O)(C)=O)C=C3)=NO1)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

References

Purity: >99.0%

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

CAY10404CAY 10404CAY-10404COXAktApoptosisCyclooxygenasePKBProtein kinase Bcyclooxygenase-2MAPKNSCLCanalgesicanti-inflammatoryanti-cancerNon-smallcelllungcancerH-1703H-358H-460Bcl-2Bcl-XLpAktpGSK-3βInhibitorinhibitorinhibit

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目录号:
HY-121537
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