An inhibitor of mutant EGFR
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Pebezertinib

Item No. 46564

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-fluoro-3-[[2-[(1-methyl-1H-pyrazol-4-yl)amino]-5-[4-(trifluoromethyl)phenyl]-4-pyrimidinyl]amino]phenyl]-2-propenamide
CAS Number
2769954-39-2
Synonyms
  • BLU-451
  • LNG-451
Molecular Formula
C24H19F4N7O
Formula Weight
497.5
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
CN1N=CC(NC2=NC(NC3=CC(NC(C=C)=O)=CC=C3F)=C(C=N2)C(C=C4)=CC=C4C(F)(F)F)=C1
InChi Code
InChI=1S/C24H19F4N7O/c1-3-21(36)31-16-8-9-19(25)20(10-16)33-22-18(14-4-6-15(7-5-14)24(26,27)28)12-29-23(34-22)32-17-11-30-35(2)13-17/h3-13H,1H2,2H3,(H,31,36)(H2,29,32,33,34)
InChi Key
XIMJCWSFLXXQMZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $41

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    10 mg

    $78

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    25 mg

    $185

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    50 mg

    $246

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    Product Description

    Pebezertinib is a covalent inhibitor of mutant EGFR.1 It selectively inhibits EGFRL858R, EGFR containing an exon 19 deletion (ex19del), and EGFR containing the exon 20 insertion D770insNGP (EGFRD770insNGP) over wild-type EGFR (IC50s = 3.4, 3, 8.6, and 81 nM, respectively). Pebezertinib reduces EGFR phosphorylation in, and the proliferation of, Ba/F3 cells expressing various EGFR mutations but does not reduce the proliferation of A431 cells, which express wild-type EGFR. It reduces tumor size in patient-derived xenograft (PDX) mouse models of non-small cell lung cancer (NSCLC) with cells expressing EGFRH773insNPH or EGFRV769insASV. Pebezertinib (2.5-25 mg/kg, p.o) reduces tumor size in a PC-9 NSCLC mouse xenograft model of metastatic brain cancer.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Millet, Y.A., Spira, A.I., Baik, C.S., et al. BLU-451, a CNS-active, potent, and selective small-molecule inhibitor against uncommon EGFR mutations. Mol. Cancer Ther. (2026).