For research use only.
CAS No. 74103-06-3
Ketorolac is a non-selective COX inhibitor of COX-1 and COX-2 with IC50 of 1.23 μM and 3.50 μM, respectively.
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|Description||Ketorolac is a non-selective COX inhibitor of COX-1 and COX-2 with IC50 of 1.23 μM and 3.50 μM, respectively.|
|Features||A COX-1 preferential inhibitor among currently marked nonsteroidal anti-inflammatory drugs (NSAIDs).|
(R, S)-, (S)-, and (R)-Ketorolac inhibit both isoforms of COX in recombinant rat and human enzyme systems, and similar as inhibitors of rat COX (rCOX) and human COX (hCOX) under the conditions used. (R, S)-Ketorolac inhibits rat COX-1, rat COX-2, human COX-1 and human COX-2 with IC50 of 0.27 μM, 2.06 μM, 1.23 μM and 3.50 μM, respectively. The (S) enantiomer of Ketorolac with IC50 of 0.10 μM for rat COX-1 is approximately twice as potent as the racemate, whereas the (R)-enantiomer with IC50 of > 100 μM is virtually without activity.  Ketorolac shows inhibition of eicosanoid formation in HEL cells (COX-1) and LPS-stimulated Mono Mac 6 cells (COX-2) with IC50 of 0.025 μM and 0.039 μM, respectively, but does not significantly inhibit NO accumulation in supernatants of LPS-stimulated RAW 264.7 cells up to 300 μM.  Ketorolac significantly inhibits thymidine incorporation of human osteoblasts (hOBs) upon 24 hours treatment in a dose-dependent manner, and inhibits proliferation and arrests cell cycle at G0/G1 phase in hOBs. 
|In vivo||(R, S)-Ketorolac is significantly more potent than indomethacin or diclofenac sodium in tests of acetic acid-induced writhing, carrageenan-induced paw hyperalgesia, and carrageenan-induced edema formation in rats, with ID50 of 0.24, 0.29 and 0.08 mg/kg, respectively.  Ketorolac produces significant inhibition of COX-1 activity and gastric PG synthesis with doses of ≥1 mg/kg inhibiting COX-1 activity by 95% and gastric PG synthesis by >88%. Ketorolac does not significantly affect COX-2 activity at doses of ≤3 mg/kg, but at doses of 10 and 30 mg/kg, Ketorolac produces significant inhibition of COX-2 activity by 75% and 91%, respectively. Ketorolac causes gastric damage in rats only at doses that inhibits both COX-1 and COX-2, or when given with a COX-2 inhibitor. |
Inhibition of Prostaglandin Formation:Recombinant COX-1 and COX-2 from rat (rCOX) and human (hCOX) expressed in a baculovirus system are purified and reconstituted with 2 mM phenol and 1 μM hematin. Then the cyclooxygenase activity is measured using a radiometric assay, and the specific activity of the final enzyme preparations used is between 20,000 and 35,000 units. Ketorolac (2 -15 μL) are diluted in DMSO and preincubated with the appropriate recombinant COX (3 -15 ng) at a final concentration of 0.01 to 1000 μM in a reaction mixture (150 μL) containing 50 mM Tris-HCl buffer (pH 7.9), 2 mM EDTA, 10% glycerol, 2 mM phenol, and 1 μM hematin for 10 minutes. The reaction is initiated by addition of [14C]arachidonic acid (50–60 mCi/mmol in a final concentration of 20 μM) and is terminated 45 seconds later by the addition of 100 μL of 0.2 N HCl and 750 μL of distilled water. The total reaction volume is then applied to a 1 mL C18 Sep-pak column that has previously been washed with 2 mL of methanol followed by 5 mL of deionized water. Oxygenated products are eluted with 3 mL of a mixture of acetonitrile/water/acetic acid (50:50:0.1, v/v/v) and quantified by liquid scintillation spectroscopy.
|In vitro||DMSO||75 mg/mL (293.8 mM)|
|Ethanol||75 mg/mL warmed (293.8 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04495894||Recruiting||Drug: Preoperative Ketorolac||Non-small Cell Lung Cancer|Renal Cell Carcinoma||Emory University||August 24 2020||Early Phase 1|
|NCT02470299||Active not recruiting||Drug: Ketorolac|Other: Placebo||Ovarian Cancer|Fallopian Tube Cancer|Peritoneal Cancer||New Mexico Cancer Care Alliance||October 29 2015||Not Applicable|
|NCT02297906||Terminated||Drug: Ketorolac||Evaluating Pharmacokinetics of Intranasal Ketorolac|Pain||Columbia University||February 2015||Phase 1|
|NCT01670799||Completed||Drug: Ketorolac||Fallopian Tube Cancer|Ovarian Cancer|Peritoneal Cavity Cancer||New Mexico Cancer Care Alliance||March 2012||Early Phase 1|
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