An irreversible inhibitor of mutant EGFRs
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Lazertinib

Item No. 29670

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[5-[[4-[4-[(dimethylamino)methyl]-3-phenyl-1H-pyrazol-1-yl]-2-pyrimidinyl]amino]-4-methoxy-2-(4-morpholinyl)phenyl]-2-propenamide
CAS Number
1903008-80-9
Synonyms
  • YH25448
Molecular Formula
C30H34N8O3
Formula Weight
554.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 3mg/mLDMF:PBS (pH 7.2) (1:2): 0.3mg/mLDMSO: 0.2mg/mL
λmax
296 nm
SMILES
COC1=C(NC2=NC=CC(N3N=C(C4=CC=CC=C4)C(CN(C)C)=C3)=N2)C=C(NC(C=C)=O)C(N5CCOCC5)=C1
InChi Code
InChI=1S/C30H34N8O3/c1-5-28(39)32-23-17-24(26(40-4)18-25(23)37-13-15-41-16-14-37)33-30-31-12-11-27(34-30)38-20-22(19-36(2)3)29(35-38)21-9-7-6-8-10-21/h5-12,17-18,20H,1,13-16,19H2,2-4H3,(H,32,39)(H,31,33,34)
InChi Key
RRMJMHOQSALEJJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $107

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    10 mg

    $160

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    25 mg

    $292

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    50 mg

    $528

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    Product Description

    Lazertinib is an irreversible inhibitor of mutant EGFRs (IC50s = 1.7, 2, and 3.3 nM for EGFRL858R/T790M, EGFRDel19/T790M, and EGFRDel19, respectively).1 It is selective for mutant EGFRs over wild-type EGFR, HER2, and HER4 (IC50s = 76, 364, and 1,017 nM, respectively). Lazertinib reduces viability of Ba/F3 cells expressing mutant EGFRs (IC50s = 3.3-5.7 nM). In vivo, lazertinib (1, 3, and 10 mg/kg) reduces tumor volume in an EGFRT790M mutant H1975 non-small cell lung cancer (NSCLC) mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yun, J., Hong, M.H., Kim, S.-Y., et al. YH25448, an irreversible EGFR-TKI with potent intracranial activity in EGFR mutant non–small cell lung cancer. Clin. Cancer Res. 25(8), 2575-2587 (2019).