Ack1 inhibitor 1 

Ack1 inhibitor 1 is a potent, selective, and orally active inhibitor of ACK1 kinase with an IC₅₀ value of 2.1 nM. Ack1 inhibitor 1 inhibits the phosphorylation of ACK1 and activation of downstream AKT. Ack1 inhibitor 1 has anti-tumor activity^[1].

Ack1 inhibitor 1 (Compound 10zi) 在 67R 和 H1975 细胞中抑制细胞生长的 IC₅₀ 分别为 3.71 μM 和 4.18 μM^[1]。
Ack1 inhibitor 1 (0 nM-5000 nM, 72 h) 在 67R 细胞中单独或与 ASK120067 联合均可增强抗肿瘤作用^[1]。
Ack1 inhibitor 1 (1 μM and 5 μM, 6 h) 呈剂量依赖性抑制 67R 细胞中 ACK1 和 AKT 的磷酸化^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Ack1 inhibitor 1 (Compound 10zi) (10 mg/kg; 口服; 单次剂量) 在SD大鼠中 AUC 值为 1920.56 h•ng/mL, C_max 值为 119.52 μg/L，生物利用度为 19.80%

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

727.77

C₃₉H₄₀F₃N₇O₄

2924415-92-7

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Li Q, et al. Design, Synthesis, and Evaluation of (R)-8-((Tetrahydrofuran-2-yl)methyl)pyrido[2,3-d]pyrimidin-7-ones as Novel Selective ACK1 Inhibitors to Combat Acquired Resistance to the Third-Generation EGFR Inhibitor. J Med Chem. 2023 May 25;66(10):6905-6921.  [Content Brief]