Ack1 Inhibitor

AIM-100 is a potent and selective Ack1 inhibitor with an IC₅₀ of 21.58 nM. AIM-100 also inhibits Tyr²⁶⁷ phosphorylation. AIM-100 does not inhibits other kinases including PI3-kinase and AKT subfamily members. AIM-100 has an anticancer effect.

(R)-9b is a potent inhibitor of ACK1 tyrosine kinase (IC₅₀=56 nM) with anticancer activity. (R)-9b exhibits selectivity for ACK1 but has inhibitory effects on JAK family kinases JAK2 and Tyk2. (R)-9b can be used in the study of hormone-regulated cancers such as prostate and breast cancer.

GNF-7 is a multikinase inhibitor. GNF-7 is a Bcr-Abl inhibitor, with IC₅₀s of 133 nM and 61 nM for Bcr-Abl^WT and Bcr-Abl^T315I, respectively. GNF-7 also possesses inhibitory activity against both ACK1 (activated CDC42 kinase 1) and GCK (germinal center kinase) with IC₅₀s of 25 nM and 8 nM, respectively. GNF-7 can be used for the research of hematologic malignancies.

KRCA-0008 is a selective ALK/Ack1 inhibitor with IC₅₀s of 12 and 4 nM for ALK and Ack1, respectively. KRCA-0008 can be used for the research of cancer.

EGFR T790M/L858R/ACK1-IN-1 is a dual inhibitor of EGFR T790M/L858R and ACK1. IC₅₀ values are 23 and 263 nM, respectively. EGFR T790M/L858R/ACK1-IN-1 can inhibit cell proliferation and has antitumor activity.

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.

Ack1 inhibitor 2 (Example 259) is an Ack1 inhibitor (IC₅₀: 0.46 μM).