A Bcr-Abl inhibitor
Related Products
Alternative(s)
10010422Nilotinib
Labeled Version(s)
19280Nilotinib-d6
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Nilotinib (hydrochloride hydrate)

Item No. 36628

Technical Information
Formal Name
4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-benzamide, monohydrochloride, monohydrate
CAS Number
923288-90-8
Molecular Formula
C28H22F3N7O • HCl [H2O]
Formula Weight
Purity
≥98%
A solid
DMF: 2 mg/mlDMSO: 3 mg/mlEthanol: 1 mg/ml
λmax
271 nm
SMILES
O=C(C1=CC=C(C)C(NC2=NC=CC(C3=CN=CC=C3)=N2)=C1)NC4=CC(C(F)(F)F)=CC(N5C=NC(C)=C5)=C4.Cl.O
InChi Code
InChI=1S/C28H22F3N7O.ClH.H2O/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);1H;1H2
InChi Key
YCBPQSYLYYBPDW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Nilotinib is an inhibitor of wild-type and mutant Bcr-Abl (IC50s = 15 and 9-400 nM, respectively).1 It is selective for wild-type and mutant Bcr-Abl over Src and LYN (IC50s = >5,000 nM for both). Nilotinib inhibits Bcr-Abl autophosphorylation and cell proliferation in Ba/F3 cells expressing wild-type or mutant Bcr-Abl (IC50s = 7-155 and 13-51 nM, respectively). In vivo, nilotinib (1 mg/kg) reduces midbrain Bcr-Abl autophosphorylation, amyloid-β levels, and neuronal loss, as well as improves autophagosome clearance and reverses cognitive deficits in the Tg2576 transgenic mouse model of Alzheimer’s disease.2 It also reduces serum creatine levels, renal profibrotic gene expression, and tubulointerstitial damage, as well as increases survival in a rat model of 5/6 nephrectomy-induced chronic kidney disease.3 Formulations containing nilotinib have been used in the treatment of leukemia.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. O'Hare, T., Walters, D.K., Stoffregen, E.P., et alIn vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants. Cancer Res. 65(11), 4500-4505 (2005).

    2. La Barbera, L., Vedele, F., Nobili, A., et alNilotinib restores memory function by preventing dopaminergic neuron degeneration in a mouse model of Alzheimer’s Disease. Prog. Neurobiol. 202, 102031 (2021).

    3. Iyoda, M., Shibata, T., Hirai, Y., et alNilotinib attenuates renal injury and prolongs survival in chronic kidney disease. J. Am. Soc. Nephrol. 22(8), 1486-1496 (2011).