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Cat. No. Name Size Price Add Cart
KI0289Nilotinib100 mg$118.8
Nilotinib200 mg$160
Nilotinib250 mg$207.9

Chemical Characteristic

Product NameNilotinib
SynonymsAMN107, Tasigna
CAS No.641571-10-0
Molecular Weight 529.52
FormulaC28H22F3N7O
Chemical Name4-methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)benzamide
SmilesC(=O)(c1cc(c(cc1)C)Nc1nc(ccn1)c1cnccc1)Nc1cc(cc(c1)C(F)(F)F)n1cnc(c1)C
Chemical Structure

Biological activities

Nilotinib inhibits the kinases BCR-ABL, KIT, LCK, EPHA3, EPHA8, DDR1, DDR2, PDGFRB, MAPK11 and ZAK.[1,2] Nilotinib (IC50 <30 nM) inhibits growth of cell lines transformed with activated KIT, PDGFR α, and PDGFR β tyrosine kinases and reduces autophosphorylation of these kinases and the ranking of affinities for these kinases is different for Nilotinib (BCR-ABL??DGFR??IT).[3] Nilotinib inhibits Ba/F3 cells (a murine hematopoietic cell line) transformed with TEL-PDGFR with an IC50 value of 18.1 nM and inhibits Ba/F3 cells transformed by a TEL-PDGFRT681I mutant with an IC50 value of 22.2 nM. Nilotinib inhibits growth of FIP1L1-PDGFR α??ransformed Ba/F3 cells at an IC50 value of 23 nM. Nilotinib (10-200 nM) treatment of FIP1L1-PDGFR α Ba/F3 cells also inhibits tyrosine autophosphorylation of FIP1L1-PDGFR α and reduces phosphorylation of its downstream signaling effector Stat5.[4] Nilotinib suppresses the growth of Ba/F3 cells transfected with the T674I mutant form of FIP1L1-PDGFRA with an inhibitory IC50 of 376 nM. Nilotinib (0.25-4 µM) induces apoptosis in FIP1L1-PDGFRA/T674I cells.[5] Nilotinib is 43 times more potent than imatinib in KBM5 (IC50 of 11.3 versus 480.5 nM) and 60 times more potent than imatinib in KBM7 (IC50 of 4.3 versus 259.0 nM) cells. IC50 for nilotinib and imatinib are 2.4 and 6.4 µM in KBM5-STI571R1.0, respectively. IC50 for nilotinib and imatinib are 97.2 nM and 2.7 µM in KBM7-STI571R1.0 cells, respectively. Besides, nilotinib inhibits autophosphorylation of Bcr-Abl kinase more effectively than imatinib in all these lines.[6] In an in vivo bone marrow transplantation assay, nilotinib (75 mg/kg/day) effectively treats myeloproliferative disease induced by TEL-PDGFR β and FIP1L1-PDGFR α, significantly increasing survival and disease latency and reducing disease severity. Nilotinib-treated (75 mg/kg/day) animals have statistically significant reductions in total white blood cells (WBCs; 563.7?109 cells/L for placebo versus 18.6?109 cells/L for AMN107) and spleen weight (802.5 mg for placebo versus 350.0 mg for AMN107).[4] In severe combined immunodeficient mice bearing KBM5 cells, mean survival times of groups treated with 10, 20, and 30 mg/kg/day of nilotinib are 144%, 159%, and 182%, respectively, compared with controls.[6]

Protocols

Nilotinib monohydrochloride stock dilutions are prepared in DMSO and stored as 10 mM solutions at -20 °C. [6]

References

[1] Weisberg E et al. AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL. Br J Cancer. 2006, 94(12): 1765-1769.
[2] Manley PW, et al. Extended kinase profile and properties of the protein kinase inhibitor nilotinib. Biochim Biophys Acta. 2010, 1804(3): 445-453.
[3] Weisberg E, et al. Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl. Cancer Cell. 2005, 7(2): 129-141.
[4] Stover EH, et al. The small molecule tyrosine kinase inhibitor AMN107 inhibits TEL-PDGFRbeta and FIP1L1-PDGFRalpha in vitro and in vivo. Blood. 2005, 106(9): 3206-3213.
[5] von Bubnoff N et al. The FIP1L1-PDGFRA T674I mutation can be inhibited by the tyrosine kinase inhibitor AMN107 (nilotinib). Blood. 2006, 107(12): 4970-4971.
[6] Golemovic M et al. AMN107, a novel aminopyrimidine inhibitor of Bcr-Abl, has in vitro activity against imatinib-resistant chronic myeloid leukemia. Clin Cancer Res. 2005, 11(13): 4941-4947.

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