alk in 9

ALK-IN-9 (compound 40) is a highly effective ALK inhibitor, demonstrating remarkable inhibitory activity against cell proliferation, with IC50 values of <0.2 nM for Ba/F3-EML4-ALK, KM 12 (TPM3-TRKA), and KG-1 cell (OP2-FGFR1).

ALK5-IN-9 is a potent, orally active inhibitor of TGFβRI (ALK5). ALK5-IN-9 inhibits ALK5 autophosphorylation (IC50: 25 nM) and inhibits NIH3T3 cell activity (IC50: 74.6 nM). ALK5-IN-9 has shown research potential in cancer diseases.

EGFR-IN-176 is an orally active and ATP-competitive inhibitor specifically targeting mutated forms of EGFR, particularly the C797S-mediated EGFR triple mutant. It effectively inhibits the activation of the AKT signaling pathway and induces apoptosis in Ba/F3 and PC-9 cells, which express EGFR19del/T790M/C797S or EGFRL858R/T790M/C797S mutations, respectively. EGFR-IN-176 selectively blocks EGFR signaling in cell lines with the EGFR triple mutation, without affecting wild-type EGFR expressed in A431 cells. Additionally, EGFR-IN-176 effectively inhibits ALK enzyme activity with an IC50 of less than 0.5 nM and is useful in the study of non-small cell lung cancer.

Ensartinib (X-396) is a potent and orally active dual ALK/MET inhibitor for the treatment of ALK-positive non-small cell lung cancer (NSCLC).