An inhibitor of EGF receptor kinase
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AG-1478

Item No. 10010244

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(3-chlorophenyl)-6,7-dimethoxy-4-quinazolinamine
CAS Number
153436-53-4
Synonyms
  • NSC 693255
  • Tyrphostin AG-1478
Molecular Formula
C16H14ClN3O2
Formula Weight
315.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1.5 mg/mlDMSO:PBS (pH 7.2) (1:8): 0.1 mg/mlEthanol: 0.5 mg/ml
λmax
222, 255, 346 nm
SMILES
COc1cc2c(ncnc2cc1OC)Nc1cccc(Cl)c1
InChi Code
InChI=1S/C16H14ClN3O2/c1-21-14-7-12-13(8-15(14)22-2)18-9-19-16(12)20-11-5-3-4-10(17)6-11/h3-9H,1-2H3,(H,18,19,20)
InChi Key
GFNNBHLJANVSQV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    AG-1478 is an inhibitor of EGFR kinase with an IC50 value of 3 nM.1 Due to its potency and selectivity, AG-1478 has been used in a broad range of studies. It reversibly inhibits rat brain Kv1.5 potassium channels (IC50 = 9.8 µM) independent of protein tyrosine kinase (PTK) activity.2 AG-1478 also inhibits the growth of leiomyoma and myometrium cell cultures with IC50 values of 5.6 and 5.7 µM, respectively.3 This inhibitor suppresses MAP kinase activation and strongly inhibits induction of fos gene expression and DNA synthesis.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Levitzki, A., and Gazit, A. Tyrosine kinase inhibition: An approach to drug development. Science 267(5205), 1782-1788 (1995).

    2. Choi, B.H., Choi, J.S., Rhie, D.J., et al. Direct inhibition of the cloned Kv1.5 channel by AG-1478, a tyrosine kinase inhibitor. Am. J. Physiol. Cell Physiol. 282, c1461-c1468 (2002).

    3. Shushan, A., Rojansky, N., Laufer, N., et al. The AG1478 tyrosine kinase inhibitor is an effective suppressor of leiomyoma cell growth. Hum. Reprod. 19(9), 1957-1967 (2004).

    4. Daub, H., Weiss, F.U., Wallasch, C., et al. Role of transactivation of the EGF receptor in signalling by G-protein-coupled receptors. Nature 379, 557-560 (1996).