Epertinib
Epertinib (S-22611) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER4 and HER2, with IC50s of 1.48 nM, 2.49 nM and 7.15 nM, respectively. Epertinib shows potent antitumor activity. Epertinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- No. CAS: 908305-13-5
- Fòrmula: C30H27ClFN5O3
- Peso molecular:560.02
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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EGFR 1.48 ± 0.0 nM (IC50) |
HER4 2.49 ± 0.1 nM (IC50) |
HER2 7.15 ± 0.5 nM (IC50) |
Epertinib inhibits the phosphorylation of EGFR and HER2 in NCI-N87 cells, with IC50 values of 4.5 and 1.6 nM, respectively[2].
Epertinib shows inhibitory activity against MDA-MB-361 cell, with an IC50 of 26.5 nM[1].
Epertinib (0-10 μM, 72 h) can selectively inhibit the proliferation of a range of cancer cell lines expressing EGFR and/or HER2[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-N87 (stomach), BT-474 (breast), SK-BR-3 (breast), MDA-MB-453 (breast), MDA-MB-175VII (breast), HT115 (colon), Calu-3 (lung), fR2 (breast), and MRC-5 (lung)
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Concentration:0-10 μM
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Incubation Time:72 h
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Result:Inhibited the growth of NCI-N87, BT-474, SK-BR-3, MDA-MB-453, MDA-MB-175VII, HT115, Calu-3, fR2, and MRC-5, with IC50 values of 8.3 ± 2.6, 9.9 ± 0.8, 14.0 ± 3.6, 48.6 ± 3.1, 21.6 ± 4.3, 53.3 ± 8.6, 241.5 ± 29.2, 5366.7 ± 65.2, and 4964.6 ± 340.3.
Epertinib (50 mg/kg, Orally, once daily for 30 days) significantly reduces the brain tumor volume[1].
Epertinib (0-50 mg/kg, Orally, once daily for 10-28 days) significantly inhibits the tumor growth in a dose-dependent manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice (BALB/cAJcl-nu/nu, implanted intracranially with MDA-MB-361 or BR2 cells)[1]
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Dosage:12.5, 25, 50, 100 mg/kg
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Administration:Orally, once daily for 28 days
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Result:Showed antitumor activity in the mammary fat pad implantation model using both cell lines and the ED50 values were comparable (24.1 mg/kg and 26.5 mg/kg for MDA-MB-361 and BR2 (MDA-MB-361-luc-BR2), respectively).
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Animal Model:Nude mice (BALB/cAJcl-nu/nu, implanted intracranially with MDA-MB-361 or BR2 cells)[1]
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Dosage:50 mg/kg
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Administration:Orally, once daily for 30 days
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Result:Significantly reduced the brain tumor volume, indicating that epertinib could have potent antitumor activity in brain metastasis even in the presence of an intact BTB (blood-tumor barrier).
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Animal Model:Nude mice (BALB/cAJcl-nu/nu, prepared by subcutaneous implantation of human gastric cancer cells, NCI-N87 into the back of nude mice)[2]
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Dosage:0, 6.25, 12.5, 25, and 50 mg/kg
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Administration:Oral gavage, daily for 10-28 days
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Result:Significantly inhibited the tumor growth in a dose-dependent manner.
Chemical Information
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No. CAS 908305-13-5
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Appearance Solid
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Peso molecular 560.02
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Fòrmula C30H27ClFN5O3
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Color Light yellow to yellow
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SMILES
CC#C/C(C1=CC2=C(NC3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=C3)N=CN=C2C=C1)=N\OC[C@@H]5NCCOC5
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Synonyms
S-22611
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. 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. [Content Brief]
[2]. 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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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