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N2567-18 Nilotinib, Free Base (AMN107) CAS: 641571-10-0

Specifications
References
CAS Number
641571-10-0
Grade
Highly Purified
Molecular Formula
C28H22F3N7O
Molecular Weight
529.52
EU Commodity Code
38220090
Shipping Temp
Blue Ice
Storage Temp
-20°C
4-Methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]benzamide; AMN107; Tasigna

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
242.5-245ºC
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°C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
Purity
~99% (by HPLC and TLC)
Form
Supplied as an off-white powder
Important Note
This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
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).
USBio References
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