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 inhibits of cell growth with IC₅₀s of 3.71 μM and 4.18 μM in 67R and H1975 cells^[1].
Ack1 inhibitor 1 (0 nM-5000 nM, 72 h) alone or in combination with ASK120067 enhances antitumor effects in 67R^[1].
Ack1 inhibitor 1 (1 μM and 5 μM, 6 h) inhibits the phosphorylation of ACK1 and AKT in 67R cells in a dose-dependent manner^[1].

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

Ack1 inhibitor 1 (Compound 10zi) (10 mg/kg; PO; single dose) improves AUC value of 1920.56 h•ng/mL, C_max of 119.52 μg/L, and an oral bioavailability of 19.80% in a single oral dose of 10 mg/kg in SD rats^[1].
. Hyzetimibe Pharmacokinetic Analysis in SD Rats ^[1]

SD大鼠体内药代动力学分析^[1]

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

727.77

C₃₉H₄₀F₃N₇O₄

2924415-92-7

CN(CC1)CCN1C(C=C2)=CC(OCC)=C2NC3=NC=C4C(N(C[C@@H]5OCCC5)C(C(C6=CC(NC(C7=CC(C(F)(F)F)=CC=C7)=O)=CC=C6)=C4)=O)=N3

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]