Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Epertinib is a reversible and selective tyrosine kinase inhibitor of EGFR, HER2, and HER4 (IC50s: 1.48 nM, 7.15 nM, and 2.49 nM). It displays a strong antitumor activity.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 6-8 weeks | $ 1,360.00 | |
50 mg | 6-8 weeks | $ 1,770.00 | |
100 mg | 6-8 weeks | $ 2,500.00 |
Description | Epertinib is a reversible and selective tyrosine kinase inhibitor of EGFR, HER2, and HER4 (IC50s: 1.48 nM, 7.15 nM, and 2.49 nM). It displays a strong antitumor activity. |
Targets&IC50 | EGFR:1.48 nM, HER2:2.49 nM, HER4:7.15 nM |
In vitro | Epertinib displays inhibitory activity against the growth of cancer cell lines expressing EGFR and/or HER2 (IC50s: 8.3 nM (NCI-N87 (stomach)), 9.9 nM (BT-474 (breast)), and 14 nM (SK-BR-3 (breast))) [1]. Epertinib 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 (IC50s: 4.5 and 1.6 nM) and it also inhibits MDA-MB-361 cell growth (IC50: 26.5 nM) [2]. |
In vivo | Epertinib displays antitumor activity in nude mice bearing NCI-N87 xenograft via oral administration for 21 days ( ED50:10.2 mg/kg). Epertinib (50 mg/kg, p.o.) is four times more potent activity than GW572016 and completely inhibits the growth of cancer cells in mice [1] and it also obviously decreases the brain tumor volume in the breast cancer intraventricular injection mouse brain metastasis model [2]. |
Synonyms | S-22611 |
Molecular Weight | 560.02 |
Formula | C30H27ClFN5O3 |
CAS No. | 908305-13-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Epertinib 908305-13-5 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors HER EGFR S 22611 S-22611 S22611 inhibitor inhibit