Epertinib

Modify Date: 2024-01-06 13:37:49

Epertinib Structure
Epertinib structure
Common Name Epertinib
CAS Number 908305-13-5 Molecular Weight 560.018
Density 1.3±0.1 g/cm3 Boiling Point 701.5±70.0 °C at 760 mmHg
Molecular Formula C30H27ClFN5O3 Melting Point N/A
MSDS N/A Flash Point 378.0±35.7 °C

 Use of Epertinib


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.

 Names

Name Epertinib
Synonym More Synonyms

 Epertinib Biological Activity

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.
Related Catalog
Target

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].
References

[1]. Tanaka H, 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. 2014 Aug;105(8):1040-8.

[2]. Tanaka Y, et al. Distribution analysis of epertinib in brain metastasis of HER2-positive breast cancer by imaging mass spectrometry and prospect for antitumor activity. Sci Rep. 2018 Jan 10;8(1):343.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 701.5±70.0 °C at 760 mmHg
Molecular Formula C30H27ClFN5O3
Molecular Weight 560.018
Flash Point 378.0±35.7 °C
Exact Mass 559.178650
LogP 6.09
Vapour Pressure 0.0±2.2 mmHg at 25°C
Index of Refraction 1.630

 Synonyms

N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-{(1Z)-N-[(3R)-3-morpholinylmethoxy]-2-butynimidoyl}-4-quinazolinamine
2-Butyn-1-one, 1-[4-[[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-6-quinazolinyl]-, O-[(3R)-3-morpholinylmethyl]oxime, (1Z)-
Epertinib
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  • Product Name: Epertinib
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  • Purity: 98.0%
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