Structure of Licofelone
CAS No.: 156897-06-2
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Licofelone is a dual COX/LOX inhibitor being considered as a treatment for osteoarthritis.
Synonyms: ML-3000
4.5
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Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
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CAS No. : | 156897-06-2 |
Formula : | C23H22ClNO2 |
M.W : | 379.88 |
SMILES Code : | O=C(O)CC1=C(C2=CC=C(Cl)C=C2)C(C3=CC=CC=C3)=C4N1CC(C)(C)C4 |
Synonyms : |
ML-3000
|
MDL No. : | MFCD00929900 |
InChI Key : | UAWXGRJVZSAUSZ-UHFFFAOYSA-N |
Pubchem ID : | 133021 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H319 |
Precautionary Statements: | P305+P351+P338 |
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
OVCAR8 | 20 µM | 72 hours | To evaluate the effect of Licofelone on reversing stem-like properties in ovarian cancer MCTS. Results showed Licofelone significantly reduced the expression of CD133, ALDH1A, KLF4, NANOG, and SOX2. | Cancer Res. 2018 Aug 1;78(15):4370-4385 |
Bone marrow cells (IMCs) | 2.5, 5, 10 μM | 5 days | To investigate the effect of Licofelone on the generation of IMCs. Results showed that Licofelone significantly suppressed the generation of Gr-1+ CD11b+ IMCs and Gr-1− F4/80+ macrophages. | Front Immunol. 2016 Dec 5;7:537 |
B16F10luc2 melanoma cells | 1, 5, 10, 20 μM | 48 hours | To evaluate the direct effect of Licofelone on melanoma cell growth and ROS production. Results showed that Licofelone had no significant effect on the viability and ROS production of B16F10luc2 melanoma cells. | Front Immunol. 2016 Dec 5;7:537 |
Colon tumor spheroids | 25 µM | 14 days | Evaluate the inhibitory effects of LFA-9 and licofelone on colon tumor spheroid formation. LFA-9 significantly inhibited colon tumor spheroid formation by 60.2%, while licofelone inhibited by 22.3%. | J Inflamm Res. 2020 Dec 31;13:1261-1278 |
Mouse peritoneal macrophages | 0.1–100 µM | 24 hours | Evaluate the inhibitory effects of LFA-9 and licofelone on PGE2 and LTB4 production in LPS-stimulated macrophages. LFA-9 inhibited PGE2 and LTB4 production, while licofelone inhibited PGE2, LTB4, and PGI2 production. | J Inflamm Res. 2020 Dec 31;13:1261-1278 |
Rat peritoneal macrophages | 0.1–100 µM | 24 hours | Evaluate the inhibitory effects of LFA-9 and licofelone on PGE2 and LTB4 production in LPS-stimulated macrophages. LFA-9 inhibited PGE2 and LTB4 production, while licofelone inhibited PGE2, LTB4, and PGI2 production. | J Inflamm Res. 2020 Dec 31;13:1261-1278 |
THP1-human monocytes | 0.1–100 µM | 24 hours | Evaluate the inhibitory effects of LFA-9 and licofelone on PGE2 and LTB4 production in LPS-stimulated macrophages. LFA-9 inhibited PGE2 and LTB4 production, while licofelone inhibited PGE2, LTB4, and PGI2 production. | J Inflamm Res. 2020 Dec 31;13:1261-1278 |
Candida albicans (CA16) | 16 mg/mL | 24 hours | Evaluate the synergistic antifungal effect of Licofelone combined with fluconazole against resistant C. albicans, showing a significant reduction in the MIC80 of fluconazole. | Front Microbiol. 2017 Nov 7;8:2101 |
Candida albicans (CA10) | 16 mg/mL | 24 hours | Evaluate the synergistic antifungal effect of Licofelone combined with fluconazole against resistant C. albicans, showing a significant reduction in the MIC80 of fluconazole. | Front Microbiol. 2017 Nov 7;8:2101 |
RAW 264.7 cells | 2.7 μM | 24 hours | To evaluate the effect of LCF-CSBN on M1 macrophage polarization, results showed that LCF-CSBN significantly reduced the expression of M1 marker iNOS and increased the expression of M2 marker CD206. | Adv Sci (Weinh). 2025 Mar;12(9):e2411911 |
A1847 | 10 µM | 72 hours | To evaluate the anti-proliferative/cell killing activity of Licofelone in ovarian cancer multicellular tumor spheroids (MCTS). Results showed Licofelone exhibited higher activity in MCTS compared to 2D cultured cells. | Cancer Res. 2018 Aug 1;78(15):4370-4385 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
Sprague Dawley rats | MIA-induced OA model and ACLT + pMMx-induced OA model | Intra-articular injection | 40 μg | Every 4 weeks for 8 weeks | To evaluate the therapeutic effect of LCF-CSBN in vivo, results showed that LCF-CSBN significantly attenuated joint inflammation, oxidative stress, and cartilage degeneration. | Adv Sci (Weinh). 2025 Mar;12(9):e2411911 |
NOD scid gamma (NSG) mice | Ovarian cancer patient-derived xenograft (PDX) model | Intraperitoneal injection | 50 mg/kg | To evaluate the effect of Licofelone in combination with paclitaxel on the survival of ovarian cancer PDX model mice. Results showed the median survival of the combination group (>141 days) was significantly longer than paclitaxel alone (115 days), licofelone alone (37 days), or vehicle (30 days). | Cancer Res. 2018 Aug 1;78(15):4370-4385 | |
C57BL/6 mice | B16F10luc2 melanoma model | Intravenous and subcutaneous injection | 5 mg/kg | Once every second day for 14 days | To evaluate the effect of Licofelone combined with a vaccine on the survival rate and immune-suppressive cell populations in melanoma-bearing mice. Results showed that Licofelone combined with the vaccine significantly prolonged the survival time of mice and reduced the number of Gr-1+ CD11b+ IMCs and Gr-1? F4/80+ macrophages in the bone marrow and spleen. | Front Immunol. 2016 Dec 5;7:537 |
Fischer (F344) rats | Carrageenan-induced rat paw edema model | Oral | 400 ppm | Single dose, measurements taken at 1-, 2-, 3-, 4-, 5- and 6-hours after carrageenan injection | Evaluate the anti-inflammatory effects of LFA-9 and licofelone on carrageenan-induced rat paw edema. LFA-9 showed 70.4% edema inhibition at 3 hours post-injection, while licofelone showed 61.7%. | J Inflamm Res. 2020 Dec 31;13:1261-1278 |
Galleria mellonella | Larvae model infected with resistant C. albicans | Injection | 80 mg/mL | Single dose, observed for 4 days | Evaluate the in vivo antifungal activity of Licofelone combined with fluconazole, showing a significant increase in larval survival rate. | Front Microbiol. 2017 Nov 7;8:2101 |
Male Sprague Dawley rats | Paclitaxel-induced mechanical allodynia model | Oral gavage | 50 mg/kg | Acute treatment, administered on day 7 or 9 after the first dose of paclitaxel | Licofelone inhibits COX and LOX and/or directly interacts with CB receptors to produce antiallodynic effects in a rat model of PINP. | Biomedicines. 2024 Jul 11;12(7):1545 |
Bovine | Early osteoarthritis model | In vitro culture | 1 mg mL−1 | 24 hours | Evaluate the uptake and retention time of Licofelone-PBAE conjugates in cartilage, showing an 18-fold increase in uptake and 37-fold prolongation in retention time. | RSC Adv. 2024 Jan 2;14(1):15-28 |
A/J mice | NNK-induced lung tumor model | Dietary administration | 200 or 400 ppm | Continued for 17 or 34 weeks | To evaluate the preventive effects of licofelone alone or in combination with DFMO on NNK-induced lung tumors. Results showed that licofelone significantly inhibited lung tumor formation, and the effect was more pronounced when combined with DFMO. | Am J Cancer Res. 2016 May 1;6(5):894-909 |
Swiss H mice | Mainstream cigarette smoke (MCS) exposure model | Dietary administration | 960 mg/kg diet | 6 weeks starting after weaning | To evaluate the early modulation by licofelone of pulmonary DNA and RNA alterations in smoke-free or MCS-exposed H mice after 10 weeks of exposure. Results showed that licofelone significantly attenuated MCS-induced DNA damage and oxidative DNA damage, and modulated the expression of various pulmonary microRNAs. | Carcinogenesis. 2020 Mar 13;41(1):91-99 |
Bio Calculators | ||||
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1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.63mL 0.53mL 0.26mL |
13.16mL 2.63mL 1.32mL |
26.32mL 5.26mL 2.63mL |
Tags: Licofelone | ML-3000 | ML3000 | ML 3000 | COX | Lipoxygenase | Apoptosis | Cyclooxygenase | LOX | inhibitor | 156897-06-2 |
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