Nilotinib hydrochloride(AMN-107 HCl) is an orally available Bcr-Abl tyrosine kinase inhibitor with antitumor activity for modulation of neuroinflammation and cognitive deficits, and may be used in studies of chronic myelogenous leukemia.

BCR-ABL:<30 nM

Nilotinib hydrochloride (AMN107 hydrochloride) is a selective Abl inhibitor designed to interact with the ATP binding site of BCR-ABL with higher affinity than imatinib while being more potent than imatinib (IC50<30 nM ), also retains activity against most BCR-ABL point mutants that confer resistance to imatinib.[1]
Nilotinib hydrochloride showed significant anti-tumor efficacy against GIST xenograft cell lines and imatinib-resistant GIST cell lines, among which the parental cell lines GK1C and GK3C showed imatinib sensitivity with IC50 of 4.59±0.97 μM and 11.15±1.48 μM, respectively.[2]

Nilotinib hydrochloride (AMN107 hydrochloride) (40 mg/kg; oral gavage; daily; for 4 weeks; BALB/cSLc-nu/nu mice with GIST xenograft) demonstrated equivalent or superior antitumor effects in BALB/cSLc-nu/nu mice with GIST xenografts. Nilotinib hydrochloride Inhibited tumor growth by 69.6% in GK1X, 85.3% in GK2X, and 47.5% in GK3X xenograft line.[2]
Nilotinib hydrochloride exerts significant healing effects on macroscopic and microscopic pathology scores in a rat model of indomethacin-induced enterocolitis and ensures considerable mucosal healing while reducing PDGFR alpha and beta levels and apoptosis in the colon Rating.[3]