| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T92057 | ||||
| Target Name | Erbb4 tyrosine kinase receptor (Erbb-4) | ||||
| Type of Target |
Successful |
||||
| Drug Potency against Target | BMS-599626 | Drug Info | IC50 = 80 nM | [1] | |
| CI-1033 | Drug Info | IC50 = 7 nM | |||
| Action against Disease Model | CI-1033 | Drug Info | The pan-ErbB inhibitor CI-1033 selectively inhibited growth of fulvestrant resistant cell lines. CI-1033 inhibited Erk but not Akt signaling, which as well as Erk is important for antiestrogen resistant cell growth | [2] | |
| References | |||||
| REF 1 | Preclinical antitumor activity of BMS-599626, a pan-HER kinase inhibitor that inhibits HER1/HER2 homodimer and heterodimer signaling. Clin Cancer Res. 2006 Oct 15;12(20 Pt 1):6186-93. | ||||
| REF 2 | Breast cancer cells can switch between estrogen receptor alpha and ErbB signaling and combined treatment against both signaling pathways postpones development of resistance. Breast Cancer Res Treat. 2010 Jun;121(3):601-13. | ||||
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