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WHI-P 154

Cat. No. 3115

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Chemical Name: 2-Bromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]phenol

Biological Activity

JAK3 inhibitor (IC₅₀ = 1.8 μM) that displays no activity at JAK1 or JAK2. Inhibits STAT1 activation, iNOS expression and NO production in macrophages in vitro. Also inhibits other common kinases including EGFR (IC₅₀ = 4 nM), Src, Abl, VEGFR, MAPK and PI 3-K and induces apoptosis in human glioblastoma cell lines (IC₅₀ = 158 μM).

Technical Data

M.Wt:

376.2

Formula:

C₁₆H₁₄BrN₃O₃

Solubility:

Soluble to 100 mM in DMSO

Purity:

>99 %

Storage:

Store at RT

CAS No:

211555-04-3

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

Narla et al (1998) 4-(3'-bromo-4'hydroxylphenyl)-amino-6,7-dimethoxyquinazoline: a novel quinazoline derivative with potent cytotoxic activity against human glioblastoma cells. Clin.Cancer Res. 4 1405. PMID: 9626456.

Changelian et al (2008) The specificity of JAK3 kinase inhibitors. Blood 111 2155. PMID: 18094329.

Sareila et al (2008) Janus kinase 3 inhibitor WHI-P154 in macrophages activated by bacterial endotoxin: differential effects on the expression of iNOS, COX-2 and TNF-α. Int.Immunopharmacol. 8 100. PMID: 18068105.

If you know of a relevant citation for this product please let us know.

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Keywords: WHI-P 154, supplier, JAK3, kinases, inhibitors, EGFR, Potent, Janus, Activated, Kinases, Epidermal, Growth, Factor, Receptors, ErbB, Her, Receptor, Tyrosine, RTKs, WHIP154