Bioactivity | MNK1/2-IN-7 (compound 20j) is an orally available inhibitor of MNK1/2 with anticancer activity and hERG safety. MNK1/2-IN-7 also inhibits the phosphorylation of eIF4E, inhibiting the MNK/eIF4E signaling pathway and cancer cell proliferation. MNK1/2-IN-7 is synergistic with Ibrutinib (HY-109970).[15][1]. |
Invitro | MNK1/2-IN-7 (1.25-5 μM; 24 h) 抑制 Hela 细胞中 eIF4E 的磷酸化 (IC50=90.5 nM) 并下调 A549 细胞中 eIF4E 和 4E-BP1 的磷酸化[1]。MNK1/2-IN-7 在人、犬、大鼠的肝脏微粒中表现出稳定性,T1/2 分别为 62.6 min,>120 min,和 64.6 min[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> MNK1/2-IN-7 相关抗体: Western Blot Analysis[1] Cell Line: |
In Vivo | MNK1/2-IN-7 (5 mg/kg; po; 单剂量) 在大鼠中表现出可接受的暴露和生物利用度,具有口服有效性[1]。MNK1/2-IN-7 (10 mg/kg; po; 17 d) 在 DOHH2 的异种异植小鼠模型中,有效使得肿瘤消退,且不影响小鼠体重。MNK1/2-IN-7 还与 Ibrutinib (HY-109970) 有协同作用[1]。在 SD 大鼠中的药代动力学分析[1]Route |
CAS | 2548283-27-6 |
Formula | C31H31N5O2 |
Molar Mass | 505.61 |
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]. Yuan X, et al. Development of an Imidazopyridazine-Based MNK1/2 Inhibitor for the Treatment of Lymphoma[J]. Journal of Medicinal Chemistry, 2024. |