An internal standard for the quantification of nilotinib
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Nilotinib-d6

Item No. 19280

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(methyl-d3)-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-5-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-benzamide-2,3,6-d3
CAS Number
1268356-17-7
Molecular Formula
C28H16D6F3N7O
Formula Weight
535.6
Purity
≥99% deuterated forms (d1-d6)
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMSO: 10 mg/ml
SMILES
O=C(NC1=CC(N2C=C(C)N=C2)=CC(C(F)(F)F)=C1)C3=C([2H])C(NC4=NC(C5=CC=CN=C5)=CC=N4)=C(C([2H])([2H])[2H])C([2H])=C3[2H]
InChi Code
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)/i1D3,5D,6D,10D
InChi Key
HHZIURLSWUIHRB-AGINCAKFSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $569

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    Product Description

    Nilotinib-d6 is intended for use as an internal standard for the quantification of nilotinib (Item Nos. 10010422 | 36628) by GC- or LC-MS. 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 al. In 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 al. Nilotinib 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 al. Nilotinib attenuates renal injury and prolongs survival in chronic kidney disease. J. Am. Soc. Nephrol. 22(8), 1486-1496 (2011).