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Medchemexpress LLC Sapitinib | 848942-61-0 | 200 MG
Supplier: Medchemexpress LLC HY13050200MG
Sapitinib (AZD-8931) is a reversible, ATP competitive EGFR inhibitor with IC50s of 4, 3, and 4 nM for EGFR, ErbB2, and ErbB3 in cells, respectively. It demonstrates potent inhibitory effects on erbB2 in ligand-independent MCF-7 cl24 cells, significantly inhibits Akt phosphorylation, and induces apoptosis in human IBC cells.
- Reversible, ATP competitive EGFR inhibitor
- Potent inhibitory effect on erbB2 in ligand-independent MCF-7 cl24 cells
- Significantly inhibits phosphorylation of Akt in SUM149 and FC-IBC-02 cells
- Inhibits proliferation and induces apoptosis in human IBC cells
- Active in xenograft tumor models responsive to EGFR inhibition alone or EGFR or erbB2 inhibition
- Causes pharmacodynamic changes in proliferation and apoptosis markers in human tumor xenograft models
- Favorable oral pharmacokinetics in rat and dog
- Low human hepatocyte turnover
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