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GW2974 is an orally active dual inhibitor of EGFR and ErbB2 (HER2) with IC50 values of 0.007 μM and 0.016 μM, respectively. It inhibits the invasion of glioblastoma multiforme (GBM) cells and tumor growth in vitro and in vivo.


| Description | GW2974 is an orally active dual inhibitor of EGFR and ErbB2 (HER2) with IC50 values of 0.007 μM and 0.016 μM, respectively. It inhibits the invasion of glioblastoma multiforme (GBM) cells and tumor growth in vitro and in vivo. |
| Targets&IC50 | HER2:0.016 μM, EGFR L858R/T790M:0.007 μM |
| In vitro | GW2974 (0.001–100 μM, 24 hours) inhibits BT474, HN5, and N87 cell growth [5]. |
| In vivo | Methods: GW2974 was administered at doses of 30 mg/kg and 100 mg/kg to a mouse model of glioblastoma multiforme (GBM) via oral administration once daily. Results: Low-dose GW2974 (30 mg/kg) inhibited intracranial tumor growth, invasion, and angiogenesis, whereas high-dose GW2974 completely reversed the low-dose suppression of tumor invasion [1]. Methods: GW2974 was administered at 10 mg/kg and 30 mg/kg via oral dosing twice daily to HN5 human tumor xenograft mouse models and BT474 human tumor xenograft mouse models. Results: GW2974 significantly inhibited tumor growth in a dose-dependent manner in both models [5]. |
| Synonyms | GW-2974, GW 2974 |
| Molecular Weight | 395.46 |
| Formula | C23H21N7 |
| Cas No. | 202272-68-2 |
| Smiles | N=1C=NC(NC=2C=CC3=C(C=NN3CC=4C=CC=CC4)C2)=C5C=C(N=CC15)N(C)C |
| Relative Density. | no data available |
| Color | Yellow |
| Appearance | Solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 16 mg/mL (40.46 mM), Sonication is recommended. | |||||||||||||||||||||||||
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