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Nilotinib
- AMN 107 - Tasigna
- Soluble in DMSO
- MF: C28H22F3N7O
- MW: 529.52
Description
Nilotinib is a potent second-generation BCR-ABL tyrosine kinase inhibitor designed to inhibit ABL1 and many imatinib-resistant BCR-ABL variants. It binds the inactive conformation of the kinase and suppresses oncogenic signaling driven by the BCR-ABL fusion protein.
Nilotinib inhibits proliferation and survival pathways downstream of BCR-ABL and is a clinically validated therapy for Philadelphia chromosome-positive chronic myeloid leukemia. It is useful for investigating kinase-inhibitor selectivity, resistance mutations and oncogene addiction in hematologic cancer models. Also available is the hydrochloride salt of Nilotinib as Axon 3168.
Key Features
- Potent second-generation BCR-ABL tyrosine kinase inhibitor
- Active against many imatinib-resistant BCR-ABL variants
- Suppresses BCR-ABL-dependent proliferation and survival signaling
- Clinically validated targeted therapy for CML
Applications
- BCR-ABL kinase pharmacology
- Chronic myeloid leukemia models
- Tyrosine kinase inhibitor resistance studies
- Oncogene addiction and apoptosis research
More Information
| Parent CAS No. | 641571-10-0 |
|---|---|
| Chemical Name | 4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino] benzamide |
| SMILES | C1C(N2C=C(C)N=C2)=CC(NC(=O)C2C=C(NC3N=C(C4C=CC=NC=4)C=CN=3)C(C)=CC=2)=CC=1C(F)(F)F |
| MFCD | MFCD09833716 |
| InChi | InChI=1S/C28H22F3N7O/c1-17-5-6-19(10-25(17)37-27-33-9-7-24(36-27)20-4-3-8-32-14-20)26(39)35-22-11-21(28(29,30)31)12-23(13-22)38-15-18(2)34-16-38/h3-16H,1-2H3,(H,35,39)(H,33,36,37) |
| InChiKey | HHZIURLSWUIHRB-UHFFFAOYSA-N |
| CID | 644241 |
| Short Description | Bcr-Abl inhibitor |
References
- H Kantarjian et al. Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL. N. Engl. J. Med. 2006, 354 (24), 2542–51.
- E Weisberg et al. AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL. Br. J. Cancer 2006, 94, 1765-1769.
- JM Goldman, JV Melo. BCR-ABL in Chronic Myelogenous Leukemia - How Does It Work? Acta Haematol. 2008, 119, 212-217.
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