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Cat. No. Name Size Price Add Cart
KI2179WHI-P15410 mg$176
WHI-P15450 mg$752

Chemical Characteristic

Product NameWHI-P154
CAS No.211555-04-3
Molecular Weight 376.2
FormulaC16H14BrN3O3
Chemical Name2-Bromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]phenol
Smilesc1(c(cc(cc1)Nc1ncnc2c1cc(c(c2)OC)OC)Br)O
Chemical Structure

Biological activities

WHI-P154 is a potent JAK3 and EGFR inhibitor. The IC50s of WHI-P154 against JAK3 and EGFR are 1.8 µM and 4 nM, respectively. WHI-P154 also significantly inhibits the activity of kinases ABL, LCK, SRC, and VEGFR with IC50s ranging from 100 nM to 1 µM.[1] In vitro, WHI-P154 inhibits the adhesion of U373 cells to laminin-coated, fibronectin-coated, collagen-coated plates with IC50s of 36.1, 29.8, 42.7 µM, respectively. WHI-P154 also inhibits the migration and invasion of human U373 glioblastoma cell in vitro.[2] In vitro, WHI-P154 at micromolar concentrations exhibits significant cytotoxicity against U373 and U87 human glioblastoma cell lines, causing apoptotic cell death. When conjugated to recombinant human epidermal growth factor (EGF), WHI-P154 shows more than 200 times antiglioblastoma activity in vitro than WHI-P154 alone and renders selective.[3] Moreover, WHI-P154 also prevents PDGF-evoked process outgrowth in human neural precursor cells in vitro.[4] In vitro assay, WHI-P154 treatment downregulates suppressor of cytokine signaling 3 (SOCS3) expression in anaplastic large cell lymphoma.[5]

Protocols

In vitro: Prior to use, WHI-P154 is dissolved in DMSO.[5]

References

[1] Changelian PS, et al. The specificity of JAK3 kinase inhibitors. Blood. 2008, 111(4): 2155-2157.
[2] Narla RK, et al. Inhibition of human glioblastoma cell adhesion and invasion by 4-(4'-hydroxylphenyl)-amino-6,7-dimethoxyquinazoline (WHI-P131) and 4-(3'-bromo-4'-hydroxylphenyl)-amino-6,7-dimethoxyquinazoline (WHI-P154). Clin Cancer Res. 1998, 4(10): 2463-2471.
[3] Narla RK, et al. 4-(3'-Bromo-4'hydroxylphenyl)-amino-6,7-dimethoxyquinazoline: a novel quinazoline derivative with potent cytotoxic activity against human glioblastoma cells. Clin Cancer Res. 1998, 4(6): 1405-1414.
[4] Richards GR, et al. The JAK3 inhibitor WHI-P154 prevents PDGF-evoked process outgrowth in human neural precursor cells. J Neurochem. 2006, 97(1): 201-210.
[5] Cho-Vega JH, et al. Suppressor of cytokine signaling 3 expression in anaplastic large cell lymphoma. Leukemia. 2004, 18(11): 1872-1878.

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