A dual inhibitor of EGFR and HER2
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Neratinib

Item No. 18404

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2E)-N-[4-[[3-chloro-4-(2-pyridinylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide
CAS Number
698387-09-6
Synonyms
  • HKI-272
Molecular Formula
C30H29ClN6O3
Formula Weight
557.0
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMF:PBS (pH7.2) (1:40): 0.02 mg/mlDMSO: 2 mg/mlEthanol: 1 mg/ml
λmax
260 nm
SMILES
CN(C/C=C/C(NC1=CC(C(NC2=CC(Cl)=C(OCC3=NC=CC=C3)C=C2)=C(C#N)C=N4)=C4C=C1OCC)=O)C
InChi Code
InChI=1S/C30H29ClN6O3/c1-4-39-28-16-25-23(15-26(28)36-29(38)9-7-13-37(2)3)30(20(17-32)18-34-25)35-21-10-11-27(24(31)14-21)40-19-22-8-5-6-12-33-22/h5-12,14-16,18H,4,13,19H2,1-3H3,(H,34,35)(H,36,38)/b9-7+
InChi Key
JWNPDZNEKVCWMY-VQHVLOKHSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

    $42

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    Product Description

    Neratinib is a dual inhibitor of EGFR and HER2 (IC50s = 92 and 59 nM, respectively).1 It is selective for EGFR and HER2 over a panel of 12 kinases (IC50s = >5,000 nM) but does inhibit VEGFR2 and Src (IC50s = 800 and 1,400 nM, respectively). Neratinib inhibits the proliferation of NCI H508 colorectal cancer cells expressing wild-type or mutant forms of HER2 (IC50s = 0.2-3 nM).2 It reduces tumor growth in BT474 breast and SKOV3 ovarian cancer mouse xenograft models when administered at a dose of 40 mg/kg.1 Formulations containing neratinib have been used in the treatment of breast cancer.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Rabindran, S.K., Discafani, C.M., Rosfjord, E.C., et al. Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase. Cancer Res. 64(11), 3958-3965 (2004).

    2. Kavuri, S.M., Jain, N., Galimi, F., et al. HER2 activating mutations are targets for colorectal cancer treatment. Cancer Discov. 5(8), 832-841 (2015).