Nilotinib is an inhibitor of wild-type and mutant Bcr-Abl (IC50s = 15 and 9-400 nM, respectively). It is selective for wild-type and mutant Bcr-Abl over Src and LYN (IC50s = >5,000 nM for both). Nilotinib inhibits Bcr-Abl autophosphorylation and cell proliferation in Ba/F3 cells expressing wild-type or mutant...

Soluble in DMSO at 50 mg/mL, very poorly soluble in ethanol, very poorly soluble in water, maximum solubility in plain water is estimated to be about 10-20 µM, buffers, serum, or other additives may increase or decrease the aqueous solubility

Nilotinib, a novel, selective BCR-ABL inhibitor, fits into the ATP-binding site of the BCR-ABL protein with higher affinity than imatinib. Nilotinib is not only more potent than imatinib against wild-type BCR-ABL (IC50 < 30nM), but also significantly active against 32/33 imatinib-resistant BCR-ABL mutants. Melting...

Soluble in DMSO or ethanol. Nilotinib is an orally bio-available aminopyrimidine-derivative Bcr-Abl tyrosine kinase inhibitor (IC(50) <30nM) with anti-neoplastic activity. Target: Abl - PDGFR - BCR , Kinase Group: RTK, PTK , Substrate: Tyrosine