A JAK3 inhibitor
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WHI-P154

Item No. 16178

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-bromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]-phenol
CAS Number
211555-04-3
Synonyms
  • JAK3 Inhibitor II
  • Janus-Associated Kinase 3 Inhibitor II
Molecular Formula
C16H14BrN3O3
Formula Weight
376.2
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 15 mg/ml
λmax
228, 247, 335 nm
SMILES
COC1=C(OC)C=C(C(NC2=CC(Br)=C(O)C=C2)=NC=N3)C3=C1
InChi Code
InChI=1S/C16H14BrN3O3/c1-22-14-6-10-12(7-15(14)23-2)18-8-19-16(10)20-9-3-4-13(21)11(17)5-9/h3-8,21H,1-2H3,(H,18,19,20)
InChi Key
CBIAKDAYHRWZCU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $90

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    10 mg

    $142

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    25 mg

    $328

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    Product Description

    WHI-P154 is a quinazoline derivative that exhibits immunosuppressive effects by selectively inhibiting JAK3 (IC50 = 1.8 μM versus IC50s > 10 μM for JAK1 and JAK2).1 It has been reported to inhibit additional kinases including EGFR (IC50 = 4 nM) and VEGFR as well as the non-receptor tyrosine kinases, Abl, Lck, and Src.1 WHI-P154 is cytotoxic to human glioblastoma cells (IC50 = 813 nM) and has been used to induce the differentiation of neuronal precursor cells.2,3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Changelian, P.S., Moshinsky, D., Kuhn, C.F., et al. The specificity of JAK3 kinase inhibitors. Blood 111(4), 2155-2157 (2008).

    2. Narla, R.K., Liu, X.P., Myers, D.E., 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. 4(6), 1405-1414 (1998).

    3. Narla, R.K., Liu, X.P., Klis, D., 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. 4(10), 2463-2471 (1998).

    4. Kim, Y.H., Chung, J.I., Woo, H.G., et al. Differential regulation of proliferation and differentiation in neural precursor cells by the Jak pathway. Stem Cells 28(10), 1816-1828 (2010).