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N-8207 Nilotinib, Free Base, >99%

[AMN-107] [Tasigna]

M.W. 529.52

C28H22F3N7O

[641571-10-0]

Storage:  Store at or below -20 ºC.  Solubility:  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.  Disposal:  A

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• 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 < 30 nM), but also significantly active against 32/33 imatinib-resistant BCR-ABL mutants.  Weisberg, E., et al.  "AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL."  Br. J. Cancer 94:  1765-1769 (2006).

• Nilotinib inhibited the proliferation of haematopoietic cells expressing the mutations in Ph+ chronic myelogenous leukemia (CML) and acute lymphoblastic leukaemia with IC50's of ~ 12 nM, thus being more potent than imatinib.  Nilotinib was also effective against several imatinib-resistant Bcr-Abl mutants, but not T315I.  Weisberg, E., et al.  "Characterization of AMN-107, a selective inhibitor of native and mutant Bcr-Abl."  Cancer Cell. 7:  129-141 (2005).

• Nilotinib and dasatinib are respectively 20-fold (IC50:  15 nM versus 280 nM) and 325-fold (IC50:  0.6 nM versus 280 nM) more potent than imatinib against cells expressing wild-type Bcr-Abl.  Similar improvements are also seen in all imatinib-resistant mutants tested, with the exception of T315I.  Thus, both inhibitors have activity against imatinib-refractory CML.  O'Hare, T., et al.  "In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants."  Cancer Res. 65:  4500-4505 (2005).

• The effects of nilotinib were studied on imatinib-sensitive (KBM5 and KBM7) and imatinib-resistant CML cell lines (KBM5-STI571R1.0 and KBM7-STI571R1.0) and were compared with those of imatinib.  The antiproliferative activity of nilotinib was 43 times more potent than that of imatinib in KBM5 cells (IC50 of 11 nM versus 480 nM) and 60 times more potent in KBM7 cells (IC50 of 4 nM versus 259 nM).  IC50's for nilotinib were 2.4 µM in KBM5-STI571R1.0 and 97 nM in KBM7-STI571R1.0 cells, while IC50's for imatinib were 6.4 µM in KBM5-STI571R1.0 and 2.5 µM in KBM7-STI571R1.0 cells.  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. 11:  4941-4947 (2005).

• Nilotinib was as potent as imatinib in inducing apoptosis (IC50 = 0.54 nM) and inhibiting proliferation (IC50 = 0.20 nM) of EOL-1 cells.  Verstovsek, S., et al.  "Activity of AMN107, a novel aminopyrimidine tyrosine kinase inhibitor, against human FIP1L1-PDGFR-alpha-expressing cells."  Leuk. Res. 30:  1499-1505 (2006).

• Nilotinib is under investigation as a possible treatment for the patients with chronic myelogenous leukemia (CML).  In June 2006, a Phase I clinical trial showed nilotinib to have a relatively favorable safety profile and to display activity in patients with CML resistant to treatment with imatinib (Gleevec®).

• Nilotinib is the active ingredient in the drug sold under the trade name Tasigna®.  This drug has been approved in at least one country for use in patients with Philadelphia chromosome-positive chronic myeloid leukemia.  NOTE:  The nilotinib sold by LC Laboratories is NOT Tasigna®, and is NOT for human use.

• Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.

• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.

• Not available in some countries; not available to some institutions; not available for some uses.