Cat. No.: HY-121537

CAY10404

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CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC₅₀ of 1 nM and a selectivity index (SI; COX-1 IC₅₀/COX-2 IC₅₀) of >500000. CAY10404 is a potent PKB/Akt and MAPK signaling pathways inhibitor and induces apoptosis in non-small cell lung cancer (NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities.

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Pureté: 99.40%
CAS No.: 340267-36-9
Formule: C₁₇H₁₂F₃NO₃S
Masse moléculaire:367.34

Stockage:

-20°C, stored under nitrogen

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

CAY10404 Chemical Structure

CAS No.: 340267-36-9

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

COX-2

1 nM (IC₅₀)

COX-1

>500 μM (IC₅₀)

Voir tous les produits spécifiques à Isoform COX :

Voir tous les produits spécifiques à Isoform Akt :

In Vitro

CAY10404 (compound 7) exhibits no inhibition of COX-1 (IC₅₀>500 µM)^[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-X_L) 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[3]

Cell Line:

Non-small cell lung cancer (NSCLC) cells (H1703, H358, H460)
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.

Western Blot Analysis^[3]

Cell Line:

NSCLC cells (H358, H460)
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-X_L) 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Chemical Information

CAS No. 340267-36-9
Appearance Solid
Masse moléculaire 367.34
Formule C₁₇H₁₂F₃NO₃S
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.
Stockage

-20°C, stored under nitrogen

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

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (272.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7223 mL

13.6114 mL

27.2227 mL

5 mM

0.5445 mL

2.7223 mL

5.4445 mL

10 mM

0.2722 mL

1.3611 mL

2.7223 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (285 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. A G Habeeb, et al. Design and synthesis of 4,5-diphenyl-4-isoxazolines: novel inhibitors of cyclooxygenase-2 with analgesic and antiinflammatory activity. J Med Chem. 2001 Aug 30;44(18):2921-7. [Content Brief]

[2]. Joshua A Robertson, et al. The role of cyclooxygenase-2 in mechanical ventilation-induced lung injury. Am J Respir Cell Mol Biol. 2012 Sep;47(3):387-94. [Content Brief]

[3]. Yongseon Cho, et al. Effects of CAY10404 on the PKB/Akt and MAPK pathway and apoptosis in non-small cell lung cancer cells. Respirology. 2009 Aug;14(6):850-8. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7223 mL	13.6114 mL	27.2227 mL	68.0568 mL
	5 mM	0.5445 mL	2.7223 mL	5.4445 mL	13.6114 mL
	10 mM	0.2722 mL	1.3611 mL	2.7223 mL	6.8057 mL
	15 mM	0.1815 mL	0.9074 mL	1.8148 mL	4.5371 mL
	20 mM	0.1361 mL	0.6806 mL	1.3611 mL	3.4028 mL
	25 mM	0.1089 mL	0.5445 mL	1.0889 mL	2.7223 mL
	30 mM	0.0907 mL	0.4537 mL	0.9074 mL	2.2686 mL
	40 mM	0.0681 mL	0.3403 mL	0.6806 mL	1.7014 mL
	50 mM	0.0544 mL	0.2722 mL	0.5445 mL	1.3611 mL
	60 mM	0.0454 mL	0.2269 mL	0.4537 mL	1.1343 mL
	80 mM	0.0340 mL	0.1701 mL	0.3403 mL	0.8507 mL
	100 mM	0.0272 mL	0.1361 mL	0.2722 mL	0.6806 mL

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CAY10404

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Voir tous les produits spécifiques à Isoform COX

Voir tous les produits spécifiques à Isoform Akt

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

CAY10404 Related Classifications

HY-121537 Related Classifications