1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR

Epertinib (Synonyms: S-22611)

Cat. No.: HY-107367
Handling Instructions

Epertinib is a potent, oral, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively; Epertinib shows potent antitumor activity.

For research use only. We do not sell to patients.

Epertinib Chemical Structure

Epertinib Chemical Structure

CAS No. : 908305-13-5

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

Epertinib is a potent, oral, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively; Epertinib shows potent antitumor activity.

IC50 & Target[1]

EGFR

1.48 nM (IC50)

HER2

2.49 nM (IC50)

HER4

7.15 nM (IC50)

In Vitro

Epertinib (S-222611) is a potent, oral, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively, and shows no effect on KDR, IGF1R, SRC, KIT, and PDGFRβ (IC50, >10000 nM). Epertinib inhibits relative phosphorylation of EGFR and HER2 in NCI-N87 cells, with IC50s of 4.5 and 1.6 nM, respectively. Furthermore, Epertinib exhibits inhibitory activity against the growth of cancer cell lines expressing EGFR and/or HER2, with IC50s of 8.3 nM (NCI-N87 (stomach)), 9.9 nM (BT-474 (breast)), and 14 nM (SK-BR-3 (breast))[1]. Epertinib also inhibits MDA-MB-361 cell growth, with an IC50 of 26.5 nM[2].

In Vivo

Epertinib shows antitumor activity in nude mice bearing NCI-N87 xenograft via oral administration for 21 days, with an ED50 of 10.2 mg/kg. Epertinib (50 mg/kg, p.o.) is four times more potent activity than lapatinib and completely inhibits the growth of cancer cells in mice[1]. Epertinib (50 mg/kg, p.o.) markedly reduces the brain tumor volume in the breast cancer intraventricular injection mouse brain metastasis model (IVM)[2].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7857 mL 8.9283 mL 17.8565 mL
5 mM 0.3571 mL 1.7857 mL 3.5713 mL
10 mM 0.1786 mL 0.8928 mL 1.7857 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

560.02

Formula

C₃₀H₂₇ClFN₅O₃

CAS No.

908305-13-5

SMILES

CC#C/C(C1=CC2=C(NC3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=C3)N=CN=C2C=C1)=N\OC[[email protected]@H]5NCCOC5

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Epertinib
Cat. No.:
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Epertinib

Cat. No.: HY-107367