A JAK3 inhibitor
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WHI-P97

Item No. 36385

Technical Information
Formal Name
2,6-dibromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]-phenol
CAS Number
211555-05-4
Synonyms
  • HY-11067
Molecular Formula
C16H13Br2N3O3
Formula Weight
Purity
≥98%
A solid
DMSO: 3.33 mg/ml
SMILES
COC1=CC2=C(N=CN=C2NC3=CC(Br)=C(C(Br)=C3)O)C=C1OC
InChi Code
InChI=1S/C16H13Br2N3O3/c1-23-13-5-9-12(6-14(13)24-2)19-7-20-16(9)21-8-3-10(17)15(22)11(18)4-8/h3-7,22H,1-2H3,(H,19,20,21)
InChi Key
YVCXQRVVNQMZEI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    WHI-P97 is an inhibitor of JAK3 (IC50 = 11 µM).1 It inhibits leukotriene C4 (LTC4) and LTB4 release, mediated by the high-affinity IgE receptor Fc ε receptor I (FcεRI), from RBL-2H3 mast cells when used at a concentration of 10 µM.2 It also inhibits FcεRI-mediated 5-lipoxygease (5-LO) translocation to the membrane in RBL-2H3 mast cells. In vivo, WHI-P97 (40 mg/kg) reduces antigen-induced LTC4 production in IgE-sensitized mice. It also reduces airway hyperresponsiveness and bronchoalveolar lavage fluid (BALF) eosinophil infiltration in a mouse model of ovalbumin-induced allergic asthma when administered at doses of 12 and 40 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sudbeck, E.A., Liu, X.P., Narla, R.K., et alStructure-based design of specific inhibitors of Janus kinase 3 as apoptosis-inducing antileukemic agents. Clin. Cancer Res. 5(6), 1569-1582 (1999).

    2. Malaviya, R., Chen, C.-L., Navara, C., et alTreatment of allergic asthma by targeting janus kinase 3-dependent leukotriene synthesis in mast cells with 4-(3', 5'-dibromo-4'-hydroxyphenyl)amino-6,7-dimethoxyquinazoline (WHI-P97). J. Pharmacol. Exp. Ther. 295(3), 912-926 (2000).