| Bioactivity | GW2974 is a potent dual inhibitor of EGFR and HER2 with IC50 value of 0.007 μM and 0.016 μM, respectively. GW2974 demonstrates in vitro inhibition of the EGFR and HER2 and inhibits the growth of tumor cell. GW2974 can be used for glioblastoma multiforme (GBM) disease research[1][2]. |
| Invitro | GW2974 (0.5-50 μM, 3小时) 10 μM 或以上时具有明显的细胞毒性，在 0.5-5 μM 时可抑制 U87MG 和 U251MG 细胞在 24 小时处理后的增殖[1]。GW2974 (0.5-5 μM, 24小时) GW2974 在 GBM 细胞侵袭和迁移中的作用与剂量有关[1]。GW2974 (0.001-100 μM, 24小时) 抑制 BT474, HN5, N87 细胞生长[2]。 0 --> GW2974 相关抗体: Cell Viability Assay[1] Cell Line: |
| In Vivo | GW2974 (30 mg/kg, 100 mg/kg,口服给药，每天一次) 在低剂量 (30 mg/kg) 对GBM 小鼠颅内肿瘤的生长、侵袭和血管生成均有抑制作用，而高剂量的 GW2974 则完全消除了低剂量 GW2974 对肿瘤侵袭的抑制作用[1]。GW2974 (10 mg/kg, 30 mg/kg,口服给药，每天两次) 在 HN5 人肿瘤异种移植小鼠模型和 BT474 人肿瘤异种移植小鼠模型中都以剂量依赖的方式显著抑制肿瘤生长[2]。 Animal Model: |
| Name | GW2974 |
| CAS | 202272-68-2 |
| Formula | C23H21N7 |
| Molar Mass | 395.46 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Wang L, et al. Differential effects of low- and high-dose GW2974, a dual epidermal growth factor receptor and HER2 kinase inhibitor, on glioblastoma multiforme invasion. J Neurosci Res. 2013 Jan;91(1):128-37. [2]. Rusnak DW, et al. The characterization of novel, dual ErbB-2/EGFR, tyrosine kinase inhibitors: potential therapy for cancer. Cancer Res. 2001 Oct 1;61(19):7196-20. |