Bioactivity | FAK-IN-9 (Compound 8f) is a potent and orally active FAK inhibitor with an IC50 of 27.44 nM. FAK-IN-9 induces triple-negative breast cancer (TNBC) cell apoptosis[1]. |
Target | IC50: 27.44 nM (FAK) |
Invitro | FAK-IN-9 (Compound 8f; 72 h) 抑制 MDA-MB-157、MDA-MB-231 和 MDA-MB-453 细胞增殖,IC50 分别为 0.167±0.025、0.126±0.012 和 0.159±0.017 μM [1]。FAK-IN-9 (1-4 μM; 72 h) 导致 MDA-MB-231 细胞以剂量依赖的方式产生相对较高水平的 NO[1]。FAK-IN-9 (1-4 μM; 48 h) 抑制 MDA-MB-231 细胞的侵袭和迁移[1]。 FAK-IN-9 (1-4 μM; 72 h) 有效阻断 FAK 介导的信号通路[1]。FAK-IN-9 (4 μM; 72 h) 抑制 MDA-MB-231 细胞局灶粘连 (FAs) 和应力纤维 (SFs) 的形成[1]。FAK-IN-9 (1-4 μM; 72 h) 诱导 MDA-MB-231 细胞凋亡[1]。 Cell Proliferation Assay[1] Cell Line: |
In Vivo | FAK-IN-9 (Compound 8f; 15 or 30 mg/kg; oral; once daily for 30 days) 抑制小鼠 MDA-MB-231 肺转移[1]。 Animal Model: |
Name | FAK-IN-9 |
CAS | 2911655-93-9 |
Formula | C36H38ClN7O8S |
Molar Mass | 764.25 |
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]. Zhang J, et al. Design, synthesis and evaluation of nitric oxide releasing derivatives of 2,4-diaminopyrimidine as novel FAK inhibitors for intervention of metastatic triple-negative breast cancer. Eur J Med Chem. 2023 Mar 15;250:115192. |