2. Immunology/Inflammation PI3K/Akt/mTOR Apoptosis
  3. COX Akt Apoptosis
  4. CAY10404

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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CAY10404 Chemical Structure

CAY10404 Chemical Structure

CAS No. : 340267-36-9

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

CAY10404 Related Antibodies

Top Publications Citing Use of Products

View All COX Isoform Specific Products:

View All Isoforms
COX COX-1 COX-2 COX-3

View All Akt Isoform Specific Products:

View All Isoforms
Akt Akt1 Akt2 Akt3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3].

IC50 & Target[1]

COX-2

1 nM (IC50)

COX-1

>500 μM (IC50)

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-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].

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

CAY10404 Related Antibodies

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-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].

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.
Molecular Weight

367.34

Formula

C17H12F3NO3S
CAS No.
Appearance

Solid

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
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)

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7223 mL 13.6114 mL 27.2227 mL
5 mM 0.5445 mL 2.7223 mL 5.4445 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (6.81 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (6.81 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.69%

SDS (393 KB)

COA (260 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CAY10404340267-36-9CAY 10404CAY-10404COXAktApoptosisCyclooxygenasePKBProtein kinase Bcyclooxygenase-2MAPKNSCLCanalgesicanti-inflammatoryanti-cancerNon-smallcelllungcancerH-1703H-358H-460Bcl-2Bcl-XLpAktpGSK-3βInhibitorinhibitorinhibit

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