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Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
Nitroxoline is an antibiotic that has proven to be very effective at combating biofilm infections. Nitroxoline is currently repurposed for the treatment of urinary tract infection, which active against susceptible gram-positive and gram-negative organisms commonly found in urinary tract infection. Nitroxoline showed a broad antimicrobial spectrum, with inhibition zone diameters and MICs of nitroxoline well below the EUCAST breakpoint for E. coli for most organisms (≤16mg/ml). Nitroxoline is active against the bacteria E. coli, S. aureus, E. faecalis, K. pneumoniae, and P. mirabilis in vitro (MIC90s = 4, 4, 8, 8, and 8 mg/L, respectively)[3]. Nitroxoline inhibits the growth of human U87 and U251 glioma, A549 lung, and PC3 prostate cancer cells (IC50s = 50, 6, 38, and 23 μg/ml, respectively)[4]. In vivo, it reduces tumor growth in a PTEN- and KRAS-driven glioma mouse model when administered at a dose of 80 mg/kg per day. Nitroxoline also inhibits the interaction between the first bromodomain of bromodomain-containing protein 4 (BRD4) with acetylated histone H4 with an IC50 value of 0.98 μM[5].
Nitroxoline/硝羟喹啉 细胞实验
Cell Line
Concentration
Treated Time
Description
References
U251 glioblastoma cells
5–80 µg/mL
4-24 hours
U251 cells were most sensitive to nitroxoline (IC50=6 mg/mL), with significant growth inhibition observed within 4 hours at 10 mg/mL.
Neuro Oncol. 2015 Jan;17(1):53-62.
L-02
0.5, 8, 4, and 1 µM
48 hours
Evaluate the cytotoxicity of ASN-1733, with an IC50 of approximately 49.61 µg/mL
Emerg Microbes Infect. 2024 Dec;13(1):2294854.
T24/CIS cells
0, 2.5, 5, 10, 20, 40 μM
24, 48, 72 hours
To evaluate the inhibitory effect of NTX on the proliferation of T24/CIS cells, results showed that NTX inhibited cell proliferation in a time- and dose-dependent manner.
Int J Biol Sci. 2021 Jul 25;17(12):3255-3267.
T24/DOX cells
0, 2.5, 5, 10, 20, 40 μM
24, 48, 72 hours
To evaluate the inhibitory effect of NTX on the proliferation of T24/DOX cells, results showed that NTX inhibited cell proliferation in a time- and dose-dependent manner.
Int J Biol Sci. 2021 Jul 25;17(12):3255-3267.
UM-UC-3
20 µM
24 hours
Evaluate migration capacity
Int J Biol Sci. 2022 Aug 8;18(13):5207-5220.
T24
10 µM
24 hours
Evaluate migration capacity
Int J Biol Sci. 2022 Aug 8;18(13):5207-5220.
J82
20 µM
48 hours
Analyze circRNA expression profile
Int J Biol Sci. 2022 Aug 8;18(13):5207-5220.
U87 glioblastoma cells
5, 10, 20, 40, 60, 80, 100 mg/mL
24 hours
Nitroxoline inhibited U87 cell proliferation in a dose-dependent manner (IC50=50 mg/mL). Low doses (5-20 mg/mL) induced G0/G1 cell-cycle arrest, while high doses (40-60 mg/mL) triggered apoptosis via caspase 3 activation and PARP cleavage.
Neuro Oncol. 2015 Jan;17(1):53-62.
Treg
300 µM
Nitroxoline significantly increased the ion-current through human K2P18.1 channels, leading to increased Treg numbers
Cell Res. 2022 Jan;32(1):72-88.
BxPC-3
41.2 μM
48 hours
Nitroxoline significantly decreased the viability of BxPC-3 cells with an IC50 value of 41.2 μM.
J Exp Clin Cancer Res. 2018 Sep 21;37(1):236.
Capan-2
16.9 μM
48 hours
Nitroxoline significantly decreased the viability of Capan-2 cells with an IC50 value of 16.9 μM.
J Exp Clin Cancer Res. 2018 Sep 21;37(1):236.
AsPC-1
26.8 μM
48 hours
Nitroxoline significantly decreased the viability of AsPC-1 cells with an IC50 value of 26.8 μM.
J Exp Clin Cancer Res. 2018 Sep 21;37(1):236.
RWPE-1
10 μM
24, 48, 72, 96 h
To evaluate the effects of Nitroxoline on the viability of RWPE-1 cells. Results showed that Nitroxoline had no significant cytotoxicity on normal RWPE-1 cells.
Int J Biol Sci. 2019 Mar 9;15(5):919-928.
PC3
10 μM
24, 48, 72, 96 h
To evaluate the effects of Nitroxoline on the viability of PC3 cells. Results showed that Nitroxoline significantly inhibited the viability of PC3 cells.
Int J Biol Sci. 2019 Mar 9;15(5):919-928.
DU145
10 μM
24, 48, 72, 96 h
To evaluate the effects of Nitroxoline on the viability of DU145 cells. Results showed that Nitroxoline significantly inhibited the viability of DU145 cells.
Int J Biol Sci. 2019 Mar 9;15(5):919-928.
LNCaP
10 μM
24, 48, 72, 96 h
To evaluate the effects of Nitroxoline on the viability of LNCaP cells. Results showed that Nitroxoline significantly inhibited the viability of LNCaP cells.
Int J Biol Sci. 2019 Mar 9;15(5):919-928.
RM9-Luc-PSA
0-50 μM
24, 48, 72, 96 h
To evaluate the effects of Nitroxoline on the viability and proliferation of RM9-Luc-PSA cells. Results showed that Nitroxoline significantly inhibited the viability and proliferation of RM9-Luc-PSA cells.
Int J Biol Sci. 2019 Mar 9;15(5):919-928.
Acanthamoeba culbertsoni
1.17 ± 0.09 µM
96 hours
Evaluation of Nitroxoline's inhibitory effect on A. culbertsoni trophozoites, IC50 of 1.17 ± 0.09 µM
Antioxidants (Basel). 2023 Dec 6;12(12):2081.
Acanthamoeba castellanii L-10
2.85 ± 0.58 µM
96 hours
Evaluation of Nitroxoline's inhibitory effect on A. castellanii L-10 trophozoites, IC50 of 2.85 ± 0.58 µM
Antioxidants (Basel). 2023 Dec 6;12(12):2081.
Acanthamoeba quina
3.24 ± 0.56 µM
96 hours
Evaluation of Nitroxoline's inhibitory effect on A. quina trophozoites, IC50 of 3.24 ± 0.56 µM
Antioxidants (Basel). 2023 Dec 6;12(12):2081.
Acanthamoeba griffini
0.69 ± 0.01 µM
96 hours
Evaluation of Nitroxoline's inhibitory effect on A. griffini trophozoites, IC50 of 0.69 ± 0.01 µM
Antioxidants (Basel). 2023 Dec 6;12(12):2081.
Acanthamoeba polyphaga
0.95 ± 0.01 µM
96 hours
Evaluation of Nitroxoline's inhibitory effect on A. polyphaga trophozoites, IC50 of 0.95 ± 0.01 µM
Antioxidants (Basel). 2023 Dec 6;12(12):2081.
Acanthamoeba castellanii Neff
0.87 ± 0.19 µM
96 hours
Evaluation of Nitroxoline's inhibitory effect on A. castellanii Neff trophozoites, IC50 of 0.87 ± 0.19 µM
Antioxidants (Basel). 2023 Dec 6;12(12):2081.
HUVEC
5 µM
72 hours
Nitroxoline induced premature senescence in HUVEC and increased p21 protein and mRNA levels.
J Natl Cancer Inst. 2010 Dec 15;102(24):1855-73.
Human umbilical vein endothelial cells (HUVEC)
1.9 µM
24 hours
Nitroxoline inhibited HUVEC proliferation with an IC50 of 1.9 µM.
J Natl Cancer Inst. 2010 Dec 15;102(24):1855-73.
Nitroxoline/硝羟喹啉 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
ICR mice
Urinary tract infection model
Oral
10 mg/kg
Two doses
Evaluate the efficacy of ASN-1733 in the urinary tract infection model, showing reduction in bacterial load in urine and bladder
Emerg Microbes Infect. 2024 Dec;13(1):2294854.
BALB/c nude mice
T24/DOX and T24/CIS subcutaneous xenograft models
Oral administration
40 mg/kg
Once daily for two weeks
To evaluate the anti-tumor effect of NTX in vivo, results showed that NTX significantly inhibited the growth of T24/DOX and T24/CIS tumors without significantly affecting mouse body weight.
Int J Biol Sci. 2021 Jul 25;17(12):3255-3267.
Mice
Genetically engineered PTEN-deleted/KRASG12D-overexpressing glioma model
Intraperitoneal injection
80 mg/kg
Daily for 14 days
Nitroxoline stabilized tumor volume (vs doubling in controls) after 14 days, increased TUNEL+ cells (15-20% vs <5%), and elevated ADC values, indicating apoptosis induction and growth suppression.
Neuro Oncol. 2015 Jan;17(1):53-62.
BALB/c nude mice
Tail vein injection model
Oral
30 mg/kg
Fed every 2 days for 8 weeks
Evaluate the inhibitory effect of Nitroxoline on bladder cancer metastasis
Int J Biol Sci. 2022 Aug 8;18(13):5207-5220.
C57BL/6 mice
Orthotopic prostate cancer model
Intragastric
15 mg/kg
On days 0, 1, 3, 4, 6, 7, 9, 10, 12, and 13 five times a week
To evaluate the antitumor effect of Nitroxoline combined with PD-1 blockade in a prostate cancer mouse model. Results showed that the combination therapy significantly suppressed tumor growth, reduced tumor weight and serum PSA levels, and enhanced antitumor immunity.
Int J Biol Sci. 2019 Mar 9;15(5):919-928.
Female athymic nude mice (BALB/c, nu/nu-NCr)
Human breast cancer xenograft model
Intraperitoneal injection
60 mg/kg
Every other day for 30 days
Nitroxoline significantly inhibited tumor growth, reducing tumor volume by 60%.
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