| Bioactivity | GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 µM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis. gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity[1]. |
| Invitro | GNE-900 (1 µM; 1-48 h) 在 HT-29 细胞中与吉西他滨 (50 nM) 联合使用时，可诱导细胞凋亡并增加裂解的 PARP 的表达[1]。 Apoptosis Analysis[1] Cell Line: |
| In Vivo | GNE-900 (2.5-40 mg/kg; p.o.; once) 与gemcitabine (HY-17026) 联用能降低肿瘤体积并增加 DNA 损伤和 γ-H2AX 的表达水平在大鼠中[1]。 Animal Model: |
| Name | GNE-900 |
| CAS | 1200126-26-6 |
| Formula | C23H21N5 |
| Molar Mass | 367.45 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Blackwood E, et al. Combination drug scheduling defines a "window of opportunity" for chemopotentiation of gemcitabine by an orally bioavailable, selective ChK1 inhibitor, GNE-900. Mol Cancer Ther. 2013 Oct;12(10):1968-80. |