AX-7396
AX-7396 (RGB-315389) is a pUL97 protein kinase inhibitor with an IC50 of 0.35 μM against HCMV pUL97 kinase. AX-7396 inhibits the replication of wild-type and agent-resistant HCMV, GPCMV, MCMV and RCMV in vitro, with the strongest potency against MCMV (IC50 1.6 μM). AX-7396 shows no significant antiviral activity in a mouse cytomegalovirus infection model. AX-7396 can be used in studies related to cytomegalovirus infection.
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- CAS. Nr.: 824431-12-1
- Formel: C15H11Cl2N3
- Molecular Weight:304.17
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
In Vitro
Ax-7396 potently inhibits HCMV pUL97 kinase activity in vitro with an IC50 of 0.35 μM, and also targets specific cellular kinases including EGFR and IGF-1R[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:primary human foreskin fibroblasts (HFFs), primary human IMR90 cells, primary mouse embryonic fibroblasts (MEFs)
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Concentration:0.1-90 μM
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Incubation Time:3, 5, or 7 days (depending on assay)
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Result:Showed no cytotoxicity in HFFs at concentrations up to 30 μM after 5 or 7 days of incubation.
Showed no notable cytotoxicity in MEFs at concentrations below 90 μM after 5 days of incubation.
Showed no significant reduction in cell viability in IMR90 cells at concentrations between 0.1 μM and 10 μM after 3 days of incubation.
Had CC50 values of 92.4 μM for HFFs (7 days) and 90.1 μM for MEFs (5 days), resulting in antiviral indices of 15.2 for HFF/HCMV and 56.3 for MEF/MCMV.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c (6-8-week-old female, mean weight ~18 g, immunocompetent, inoculated i.p. with 5×105 PFU mouse cytomegalovirus strain Smith)[2]
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Dosage:50 mg/kg
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Administration:i.p.; on days -1, 1, 4, and 7 relative to infection
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Result:Resulted in a slight, non-significant reduction of infectious viral titers in salivary glands compared to placebo-treated controls.
Showed no significant inhibition of viral genomic loads in salivary glands, spleens, livers, or lungs relative to placebo.
Chemical Information
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CAS. Nr. 824431-12-1
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Molecular Weight 304.17
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Formel C15H11Cl2N3
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SMILES
ClC1=CC=C(NC2=C3C=C(C)C=CC3=NC=N2)C=C1Cl
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Synonyms
RGB-315389
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Breza N, et al. Synthesis and characterization of novel quinazoline type inhibitors for mutant and wild-type EGFR and RICK kinases. Journal of receptor and signal transduction research. 2008;28(4):361-73. [Content Brief]
[2]. Schleiss M, et al. Protein kinase inhibitors of the quinazoline class exert anti-cytomegaloviral activity in vitro and in vivo. Antiviral research. 2008 Jul;79(1):49-61. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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