A potent inhibitor of mutant EGFRs
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EAI045

Item No. 19719

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-1-oxo-N-2-thiazolyl-2H-isoindole-2-acetamide
CAS Number
1942114-09-1
Molecular Formula
C19H14FN3O3S
Formula Weight
383.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlEthanol: 1 mg/mlPBS (pH 7.2): 0.1 mg/ml
λmax
203, 270 nm
SMILES
FC1=CC=C(C(C(N2CC(C=CC=C3)=C3C2=O)C(NC4=NC=CS4)=O)=C1)O
InChi Code
InChI=1S/C19H14FN3O3S/c20-12-5-6-15(24)14(9-12)16(17(25)22-19-21-7-8-27-19)23-10-11-3-1-2-4-13(11)18(23)26/h1-9,16,24H,10H2,(H,21,22,25)
InChi Key
YTUFHOKUFOQRDF-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

    EAI045 is a potent and selective inhibitor of mutant EGF receptors (EGFRs; IC50s = 0.076, 0.049, 0.002, and 1.6 μM for recombinant EGFRL858R, EGFRT790M, EGFRL858R/T790M, and wild-type EGFR, respectively).1 It inhibits phosphorylation of EGFR in a concentration-dependent manner in H1975 cells. EAI045 (0.01-10 μM) reduces proliferation of Ba/F3 cells expressing EGFRL858R/T790M and EGFRL858R/T790M/I941R. In vivo, EAI045 induces tumor regression and reduces EGFR signaling in mice bearing EGFRL858R/T790M, EGFRExon19del/T790M, and EGFRL858R/T790M/C797S tumors when administered at a dose of 60 mg/kg per day in combination with cetuximab.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jia, Y., Yun, C.H., Park, E., et al. Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors. Nature 534(7605), 129-132 (2016).