Home  >  Products  >  Nilotinib, Free Base (4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide, AMN-107, Tasigna)

Nilotinib, Free Base (4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide, AMN-107, Tasigna)

Cat no: N2567-18


Supplier: United States Biological
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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 < 30nM), but also significantly active against 32/33 imatinib-resistant BCR-ABL mutants. Melting Point: 242.5-245C Solubility: Soluble in DMSO at 50mg/ml; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-20uM; buffers, serum, or other additives may increase or decrease the aqueous solubility. Elemental Analysis: Calculated C - 63.51% H - 4.19% F - 10.76% N - 18.52% Storage and Stability: May be stored at RT for short-term only. Long-term storage is recommended at -20 degrees C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
Catalogue number: N2567-18
Size: 25mg
Form: Supplied as an off-white powder
Purity: ~99% (by HPLC and TLC)
References: 1. Weisberg, E., et al. "AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL." Br. J. Cancer 94:1765-1769 (2006). 2. Weisberg, E., et al. "Characterization of AMN-107, a selective inhibitor of native and mutant Bcr-Abl." Cancer Cell. 7:129-141 (2005). 3. 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). 4. 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). 5. 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).

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