1. Immunology/Inflammation Apoptosis
  2. COX Apoptosis
  3. Ketorolac

Ketorolac (RS37619) is a non-steroidal anti-inflammatory drug (NSAID), acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2. Ketorolac tromethamine is used as 0.5% ophthalmic solution for the research of allergic conjunctivitis, cystoid macular edema, intraoperative miosis, and postoperative ocular inflammation and pain. Ketorolac tromethamine is also a DDX3 inhibitor that can be used for cancer research.

For research use only. We do not sell to patients.

Ketorolac

Ketorolac Chemical Structure

CAS No. : 74103-06-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Ketorolac (RS37619) is a non-steroidal anti-inflammatory drug (NSAID), acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2. Ketorolac tromethamine is used as 0.5% ophthalmic solution for the research of allergic conjunctivitis, cystoid macular edema, intraoperative miosis, and postoperative ocular inflammation and pain. Ketorolac tromethamine is also a DDX3 inhibitor that can be used for cancer research[1][4].

IC50 & Target[1]

COX-1

20 nM (IC50)

COX-2

120 nM (IC50)

DDX3

 

Cellular Effect
Cell Line Type Value Description References
A549 IC50
13 μM
Compound: Toradol
Inhibition of PAK1/COX2 in human A549 cells harboring Ki-RAS mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay
Inhibition of PAK1/COX2 in human A549 cells harboring Ki-RAS mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 27889630]
A549 IC50
36 μM
Compound: Toradol
Inhibition of PAK1 in human A549 cells using myelin basic protein as substrate preincubated for 24 hrs followed by PAK1 immunoprecipation and substrate addition measured after 60 mins by ATP-Glo kinase assay
Inhibition of PAK1 in human A549 cells using myelin basic protein as substrate preincubated for 24 hrs followed by PAK1 immunoprecipation and substrate addition measured after 60 mins by ATP-Glo kinase assay
[PMID: 27889630]
B16-F10 IC50
30 μM
Compound: Toradol
Cytotoxicity against PAK1-independent mouse B16F10 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Cytotoxicity against PAK1-independent mouse B16F10 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 27889630]
In Vitro

Ketorolac (RS37619) salt (0-30 μM; 48 h) effectively kills the oral cancer cells[4].
Ketorolac salt (0-5 μM; 48 h) inhibits the expression of DDX3 protein, and induces apoptosis in H357 cells[4].
Ketorolac salt (0-2.5 μM; 0-16 h) inhibits the proliferation of oral cancer cells[4].
Ketorolac salt (0-50 μM) directly interacts with DDX3 and inhibits the ATPase activity[4].

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

Cell Viability Assay[4]

Cell Line: HOK, SCC4, SCC9 and H357 cells
Concentration: 0-30 μM
Incubation Time: 48 h
Result: Showed inhibition with IC50s of 2.6, 7.1 and 8.1 μM against H357, SCC4 and SCC9 cells, respectively. And the normal HOK cell line did not show any cell death effect.

Cell Proliferation Assay[4]

Cell Line: H357
Concentration: 0.5, 1.0, 1.5, 2.0 and 2.5 μM
Incubation Time: 0, 8 and 16 h
Result: Inhibited the proliferation.

Western Blot Analysis[4]

Cell Line: H357
Concentration: 1, 2.5 and 5 μM
Incubation Time: 48 h
Result: Significantly reduced DDX3 protein expression levels, but not completely ablated as compared to DMSO treated cells. Up regulated the expression of E-cadherin.

Apoptosis Analysis[4]

Cell Line: H357
Concentration: 2.5 and 5 μM
Incubation Time: 48 h
Result: Induced apoptosis.
In Vivo

Ketorolac (RS37619) (0.4% ketorolac tromethamine ophthalmic solution) shows powerful ocular anti-inflammatory activities in rabbits[1].
Ketorolac (4 mg/kg/day, p.o.; 2 weeks) has no detrimental effect in the volume fraction of bone trabeculae formed inside the alveolar socket in rats[2].
Ketorolac (60 μg; intrathecal injection; once) attenuates the damage caused by spinal cord ischemia in rats[3].
Ketorolac salt (20 and 30 mg/kg; i.p.; two times in a week for 3 weeks) reduces oral carcinogenesis in mice[4].

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

Animal Model: New Zealand White rabbits (2.0–2.7 kg), LPS endotoxin-induced ocular inflammation[1]
Dosage: 50 μL ketorolac tromethamine ophthalmic solution 0.4%
Administration: In eyes, twice, 2 hours and 1 hour before LPS challenge
Result: Resulted in a nearly complete inhibition (98.7%) of LPS endotoxin-induced increases in FITC (fluorescein isothiocyanate)-dextran in the anterior chamber, and resulted in a nearly complete inhibition (97.5%) of LPS endotoxin-induced increases in aqueous PGE2 concentrations in the aqueous humor.
Animal Model: Male Wistar rats (400–450 g), spinal cord ischemia model[3]
Dosage: 30 and 60 μg
Administration: Intrathecal injection, 1 h before the ischemia induction for once
Result: Significantly reduced the motor disturbances and improved the survival rate at 60 μg.
Animal Model: Significantly reduced the motor disturbances and improved the survival rate at 60 μg.
Dosage: 20 mg/kg and 30 mg/kg
Administration: IP injection, two times in a week for 3 weeks
Result: Decreased tumor burden, reduced expression of DDX3 and anti-apoptotic proteins (Bcl-2 and Mcl-1).
Clinical Trial
Molecular Weight

255.27

Formula

C15H13NO3

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1C2=CC=C(C(C3=CC=CC=C3)=O)N2CC1)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (783.48 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 3.9174 mL 19.5871 mL 39.1742 mL
5 mM 0.7835 mL 3.9174 mL 7.8348 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 (sealed storage, away from moisture). 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
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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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: ≥ 5 mg/mL (19.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (19.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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 (sealed storage, away from moisture)

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: 99.87%

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 (sealed storage, away from moisture). 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 3.9174 mL 19.5871 mL 39.1742 mL 97.9355 mL
5 mM 0.7835 mL 3.9174 mL 7.8348 mL 19.5871 mL
10 mM 0.3917 mL 1.9587 mL 3.9174 mL 9.7936 mL
15 mM 0.2612 mL 1.3058 mL 2.6116 mL 6.5290 mL
20 mM 0.1959 mL 0.9794 mL 1.9587 mL 4.8968 mL
25 mM 0.1567 mL 0.7835 mL 1.5670 mL 3.9174 mL
30 mM 0.1306 mL 0.6529 mL 1.3058 mL 3.2645 mL
40 mM 0.0979 mL 0.4897 mL 0.9794 mL 2.4484 mL
50 mM 0.0783 mL 0.3917 mL 0.7835 mL 1.9587 mL
60 mM 0.0653 mL 0.3265 mL 0.6529 mL 1.6323 mL
80 mM 0.0490 mL 0.2448 mL 0.4897 mL 1.2242 mL
100 mM 0.0392 mL 0.1959 mL 0.3917 mL 0.9794 mL
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  • 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.

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Ketorolac
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