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 Chemical Structure

Ketorolac Chemical Structure

CAS No. : 74103-06-3

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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

 

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

White to light 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 : 250 mg/mL (979.36 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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Working solution concentration: mg/mL
Purity & Documentation
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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