zapnometinib

SKU: orb1940242

Description

zapnometinib is a MEK inhibitor.(In Vitro):Zapnometinib inhibits MEK, with IC50s of 30.96 nM, 357 nM, and 15 nM in cell free kinase assay, A549, MDCK cells and human PBMCs.Zapnometinib reduces the viral titers of the IV H1N1pdm09, H3N2.(In Vivo):Zapnometinib exhibits AUC values of 860.02 and 1953.68 μg h/mL in mice by i.v. or oral route, respectively.Zapnometinib reduces the lung virus titers and enhances survival of mice after lethal H1N1pdm09 infection.

Key Properties

• CAS Number: 303175-44-2
• MW: 409.55
• Purity: >98% (HPLC)
• Formula: C₁₃H₇ClF₂INO₂
• SMILES: OC(c(c(Nc(ccc(I)c1)c1Cl)c1F)ccc1F)=O
• Target: Influenza Virus
• Solubility: In Vitro: DMSO : 62.5 mg/mL (152.61 mM)

Bioactivity

• In Vivo:
  Animal model: Female C57BL/6 mice (8 weeks; 21-24 g) were infected with H1N1pdm09. Dosage: 8.4, 25, 75 mg/kg/day (2.8, 8.4, 25 mg/kg). Administration: p.o. three times a day. Result: Significantly reduced the virus titer at the dose of either 75 mg/kg/day or 25 mg/kg/day.
• In Vitro:
  Western blot analysis. Cell line: human PBMCs. Concentration: 100 μM. Incubation time: 4 h. Result: Inhibited the Ionomycin (PMA/I)-increased pERK1/2.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

2-(2-chloro-4-iodoanilino)-3,4-difluorobenzoic acid | PD0184264 | ATR-002

Quick Database Links

Gene Symbol

Influenza Virus