| Name | Zafirlukast |
| Description | Zafirlukast (ICI 204219) is an orally active leukotriene D4 receptor (LTD4) antagonist (IC50=0.6 μM). Zafirlukast has anti-asthmatic, anti-inflammatory, and antimicrobial properties and is used in the prevention and treatment of asthma. |
| In vitro | METHODS: Loucy cells were treated with THZ1 (0.8-500 nM) for 4 h. Binding was detected by LanthaScreen Eu Kinase Binding assay.
RESULTS: THZ1 showed time-dependent inhibition of CDK7 in vitro and covalent binding of intracellular CDK7. [1]
METHODS: NSCLC cell lines H1299, A549 and H292 were treated with THZ1 (10-10000 nM) for 48 h. Cell viability was measured by crystal violet assay.
RESULTS: THZ1 dose-dependently inhibited the migration and proliferation of NSCLC cells. [2] |
| In vivo | METHODS: To detect anti-tumor activity in vivo, THZ1 (10 mg/kg) was injected intravenously twice daily for 28 days into NU/NU mice bearing MYCN-amplified human NB xenografts.
RESULTS: THZ1 inhibited tumor growth in the human MYCN-amplified NB mouse model. [3]
METHODS: To detect the antitumor activity in vivo, THZ1 (10 mg/kg) was injected intraperitoneally into NSG mice bearing KYSE510 tumors twice daily for 24 days.
RESULTS: THZ1 inhibited the growth of KYSE510 xenografts and suppressed lung metastasis in the NSG mouse model. [4] |
| Storage | keep away from direct sunlight,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 55 mg/mL (95.54 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | Leukotriene Receptor | ICI204219 | ICI-204219 | Inhibitor | inhibit | Zafirlukast |
| Inhibitors Related | Montelukast sodium | L 651896 | L 674573 | REV 5901A | Pranlukast | Montelukast | CGP 35949 | ABT-080 | MK-571 sodium | Masilukast |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Viral Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | GPCR Compound Library |
United States
