A selective antagonist of the EGFR
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EGFR Inhibitor

Item No. 15363

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[[6-[[3-(trifluoromethyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]-cyclopropanecarboxamide
CAS Number
879127-07-8
Synonyms
  • Epidermal Growth Factor Receptor Inhibitor
  • ErbB-1 Inhibitor
  • HER1 Inhibitor
Molecular Formula
C21H18F3N5O
Formula Weight
413.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 20 mg/mlDMSO:PBS(pH 7.2) (1:3): 0.25 mg/mlEthanol: 0.2 mg/ml
λmax
253, 302 nm
SMILES
O=C(C1CC1)NC2=CC=CC(NC3=CC(NC4=CC(C(F)(F)F)=CC=C4)=NC=N3)=C2
InChi Code
InChI=1S/C21H18F3N5O/c22-21(23,24)14-3-1-4-15(9-14)27-18-11-19(26-12-25-18)28-16-5-2-6-17(10-16)29-20(30)13-7-8-13/h1-6,9-13H,7-8H2,(H,29,30)(H2,25,26,27,28)
InChi Key
YOHYSYJDKVYCJI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $103

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    Product Description

    EGFR inhibitor is a cell permeable, 4,6-disubstituted pyrimidine compound that selectively inhibits the EGFR kinase with an IC50 value of 21 nM in vitro and blocks receptor autophosphorylation in cells.1 It can also inhibit the L858R and L861Q EGFR mutants (IC50s = 63 and 4 nM, respectively) yet displays strong selectivity for EGFR against a panel of 55 recombinant kinases (IC50s > 10 μM).1 Whereas overactivity of EGFR tyrosine kinases has been associated with a number of cancers, inhibition of EGFR has been shown to induce apoptosis by downregulating antiapoptotic proteins such as survivin and upregulating proapoptotic proteins such as Bim.2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zhang, Q., Liu, Y., Gao, F., et al. Discovery of EGFR selective 4,6-disubstituted pyrimidines from a combinatorial kinase-directed heterocycle library. J. Am. Chem. Soc. 128(7), 2182-2183 (2006).

    2. Ciardiello, F., and Tortora, G. EGFR antagonists in cancer treatment. N. Engl. J. Med. 358(11), 1160-1174 (2008).

    3. Okamoto, K., Okamoto, I., Okamoto, W., et al. Role of survivin in EGFR inhibitor-induced apoptosis in non-small cell lung cancers positive for EGFR mutations. Cancer Res. 70(24), 10402-10410 (2010).