NeladalkibTFA is the TFA salt form of Neladalkib. Neladalkib (NVL-655) is an orally available ALK inhibitor, exhibiting an IC50 of 2.8 nM against ALK. It induces apoptosis and demonstrates antitumor activity.

Neladalkib TFA exhibits an IC50 of 2.7 nM in Ba/F3 CLIP1-LTK cells. It demonstrates strong inhibitory effects on various ALK mutations, including ALK T1151insT, ALK T1151M, ALK L1152R, ALK C1156Y, ALK I1171N, ALK I1171S, ALK I1171T, ALK F1174L, ALK F1174S, ALK V1180L, ALK L1198F, ALK G1202R, ALK D1203N, ALK S1206R, and ALK R1275Q, with IC50 values ranging from 0.9 to 6.8 nmol/L. In contrast, it shows weaker inhibition against ALK G1196M, ALK G1269A, and ALK G1269S, with IC50 values between 11 and 79 nmol/L. Additionally, Neladalkib (1-100 nM, 24 h) TFA increases caspase 3/7 activation and decreases S phase cells, promoting apoptosis in NCI-H3122 cells.

Neladalkib (0.06-1.5 mg/kg, orally, twice daily, for 0-28 days) TFA exhibits antitumor activity in mice.