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Tyrphostin AG 879 potently inhibits HER2/ErbB2 with IC50 of 1 μM, 100- and 500-fold higher selective to ErbB2 than PDGFR and EGFR.
| Cell Experiment | |
|---|---|
| Cell lines | MCF-7 cells |
| Preparation method | Growing cells in 96-well plates which is containing 100 μL medium per well. Ten microliters of MTT solution (5 mg/ml in PBS) is added to each well and incubation continued for 4 h at 37 °C. Subsequently, 100 μL 10% SDS in 0.01 M HCl is added. After incubation at 37°C overnight, absorption is measured at 550 nm in an ELISA reader using a reference filter of 690 nm. |
| Concentrations | 20 μM |
| Incubation time | 46 hours |
| Animal Experiment | |
|---|---|
| Animal models | nude mice carrying v-Ha-RAS transformed NIH 3T3 cells |
| Formulation | 30% dimethyl sulfoxide with PBS |
| Dosages | 20 mg/kg |
| Administration | Intraperitoneally administrated on days 3, 5, 7, 10, 12, 14, and 17. |
| Molecular Weight | 316.46 |
| Formula | C18H24N2OS |
| CAS Number | 148741-30-4 |
| Solubility (25°C) | DMSO 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related EGFR/HER2 Products |
|---|
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| Sapitinib (AZD8931)
AZD8931 (Sapitinib) is an equipotent, reversible inhibitor of Signaling by EGFR, ERBB2 (HER2), and ERBB3 with IC50 of 4, 3, 4 nM respectively. |
| Afatinib
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| CP-724714
CP-724714 is a potent and selective orally active HER-2 tyrosine kinase inhibitor, IC50 = 3 nM. |
| Erlotinib Hydrochloride
Erlotinib is an inhibitor of human EGFR tyrosine kinase (IC50 = 2 nM) and decreases EGFR autophosphorylation in tumor cells (IC50 = 20 nM). |
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