An inhibitor of EGFR, HER2, and HER4
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Epertinib (hydrochloride)

Item No. 44442

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[4-[[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-6-quinazolinyl]-2-butyn-1-one, O-[(3R)-3-morpholinylmethyl]oxime, monohydrochloride
CAS Number
2071195-74-7
Synonyms
  • S-222611
Molecular Formula
C30H27ClFN5O3 • HCl
Formula Weight
596.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/ml
SMILES
FC1=CC=CC(COC(C=CC(NC2=NC=NC3=C2C=C(C=C3)/C(C#CC)=N/OC[C@@H]4NCCOC4)=C5)=C5Cl)=C1.Cl
InChi Code
InChI=1S/C30H27ClFN5O3.ClH/c1-2-4-27(37-40-18-24-17-38-12-11-33-24)21-7-9-28-25(14-21)30(35-19-34-28)36-23-8-10-29(26(31)15-23)39-16-20-5-3-6-22(32)13-20;/h3,5-10,13-15,19,24,33H,11-12,16-18H2,1H3,(H,34,35,36);1H/b37-27+;/t24-;/m1./s1
InChi Key
NVWJPQQXBPWOOA-PLXRJBJVSA-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

    Epertinib is an inhibitor of EGFR, HER2, and HER4 (IC50s = 1.48, 7.15, and 2.49 nM, respectively).1 It is selective for these kinases over VEGFR2, insulin-like growth factor 1 receptor (IGF-1R), c-Src, KIT, and PDGFRβ (IC50s = >10,000 nM for all). Epertinib inhibits EGFR and HER2 autophosphorylation in NCI N87 gastric carcinoma cells (IC50s = 4.5 and 1.6 nM, respectively). It selectively inhibits the growth of NCI N87, BT474 breast, and HT115 colon carcinoma cancer cell lines (IC50s = 8.3, 9.9, and 53.3 nM, respectively) over fR2 breast epithelial cells and MRC-5 fibroblasts (IC50s = 5,366.7 and 4,964.6 nM, respectively). Epertinib (12.5 or 50 mg/kg per day) decreases tumor volume in an NCI N87 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tanaka, H., Hirata, M., Shinonome, S., et al. Preclinical antitumor activity of S-222611, an oral reversible tyrosine kinase inhibitor of epidermal growth factor receptor and human epidermal growth factor receptor 2. Cancer Sci. 105(8), 1040-1048 (2014).