A multi-kinase inhibitor
Related Products
Alternative(s)
23452WHI-P180
Isomer(s)
10011246WHI-P131
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

WHI-P180 (hydrochloride)

Item No. 44365

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[(6,7-dimethoxy-4-quinazolinyl)amino]-phenol, monohydrochloride
CAS Number
153437-55-9
Molecular Formula
C16H15N3O3 • HCl
Formula Weight
333.8
Purity
≥95%
Formulation (Request formulation change)
A solid
SMILES
COC1=CC2=NC=NC(NC3=CC(O)=CC=C3)=C2C=C1OC.Cl
InChi Code
InChI=1S/C16H15N3O3.ClH/c1-21-14-7-12-13(8-15(14)22-2)17-9-18-16(12)19-10-4-3-5-11(20)6-10;/h3-9,20H,1-2H3,(H,17,18,19);1H
InChi Key
MJLLZROGIFJFJJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    5 mg

    $40

    Add

    10 mg

    $75

    Add

    25 mg

    $149

    Add

    50 mg

    $278

    Add
    Kinase Resource Center
    Discover Products & Resources for Kinase Research
    • Kinase inhibitors, screening libraries, assay kits, & more
    • Tools to study kinase signaling pathways:
      • Growth factor signaling
      • PI3K/Akt/mTOR
      • MAPKs (ERK, p38, & JNK)
      • JAK/STAT signaling
    • Articles, resources, & advice
    EXPLORE NOW
    Product Description

    WHI-P180 is a multi-kinase inhibitor with IC50 values of 4.5 and 66 nM for the human proto-oncogene RET and kinase insert domain receptor (KDR), respectively.1 It also inhibits EGFR (IC50 = 4 μM) and binds to tau-tubulin kinase 1 (TTBK1; Kds = 0.46 and 0.24 μM for phosphorylated and non-phosphorylated TTBK1, respectively).2,3 WHI-P180 inhibits JAK3 and JAK3-driven graft versus host disease responses in mice receiving allogenic bone marrow and splenocyte grafts.2,4 WHI-P180 (25 mg/kg, i.p) inhibits IgE-induced vascular hyperpermeability in a mouse model of passive anaphylaxis.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Newton, R., Bowler, K.A., Burns, E.M., et al. The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity. Eur. J. Med. Chem. 13, 20-32 (2016).

    2. Ghosh, S., Jennissen, J.D., Liu, X.P., et al. 4-[3-Bromo-4-hydroxyphenyl)amino]-6,7-dimethoxyquinazolin-1-ium chloride methanol solvate and 4-[(3-hydroxyphenyl)amino]-6,7-dimethoxy-1-quinazolinium chloride. Acta. Crystallogr. C. 57(Pt 1), 76-78 (2001).

    3. Xue, Y., Wan, P.T., Hillertz, P., et al. X-ray structural analysis of tau-tubulin kinase 1 and its interactions with small molecular inhibitors. ChemMedChem 8(11), 1846-1854 (2013).

    4. Cetkovic-Cvrlje, M., Roers, B.A., Schonhoff, D., et al. Treatment of post-bone marrow transplant acute graft-versus-host disease with a rationally designed JAK3 inhibitor. Leuk. Lymphoma. 43(7), 1447-1453 (2002).

    5. Chen, C.-L., Malaviya, R., Navara, C., et al. Pharmacokinetics and biologic activity of the novel mast cell inhibitor, 4-(3-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline in mice. Pharm. Res. 16(1), 117-122 (1999).