An irreversible inhibitor of EGFR kinase activity
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CL 387,785

Item No. 19081

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[(3-bromophenyl)amino]-6-quinazolinyl]-2-butynamide
CAS Number
194423-06-8
Synonyms
  • EKB-785
  • EKI-785
  • WAY-EKI-785
Molecular Formula
C18H13BrN4O
Formula Weight
381.2
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMF:PBS (pH 7.2) (1:4): 0.2 mg/mlDMSO: 5 mg/ml
λmax
246, 317, 348 nm
SMILES
BrC1=CC(NC2=NC=NC3=C2C=C(NC(C#CC)=O)C=C3)=CC=C1
InChi Code
InChI=1S/C18H13BrN4O/c1-2-4-17(24)22-14-7-8-16-15(10-14)18(21-11-20-16)23-13-6-3-5-12(19)9-13/h3,5-11H,1H3,(H,22,24)(H,20,21,23)
InChi Key
BTYYWOYVBXILOJ-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

    CL 387,785 is a potent, irreversible inhibitor of EGFR kinase activity (IC50 = 370 pM).1 It blocks EGF-stimulated autophosphorylation of receptors in cells (IC50 = 5 nM) and halts cell cycling in cells that overexpress EGFR or c-ErbB2 (IC50s = 31-125 nM).1 CL 387,785 profoundly blocks the growth of EGFR-overexpressing tumors in nude mice when given orally at 80 mg/kg/day for 10 days.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Discafani, C.M., Carroll, M.L., Floyd, M.B., Jr., et al. Irreversible inhibition of epidermal growth factor receptor tyrosine kinase with in vivo activity by N-[4-[(3-bromophenyl)amino]-6-quinazolinyl]-2-butynamide (CL-387,785). Biochem. Pharmacol. 57(8), 917-925 (1999).