<Suppliers Price>

Nilotinib hydrochloride anhydrous

Names

[ CAS No. ]:
923288-95-3

[ Name ]:
Nilotinib hydrochloride anhydrous

[Synonym ]:
Benzamide, 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-, hydrochloride (1:1)
4-Methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluormethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzolcarboxamidhydrochlorid
4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide hydrochloride
Nilotinib hydrochloride anhydrous
X8407
4-méthyl-N-[3-(4-méthyl-1H-imidazol-1-yl)-5-(trifluorométhyl)phényl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide chlorhydrate
benzamide, 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-, monohydrochloride
Nilotinib hydrochloride
4-Methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-{[4-(3-pyridinyl)-2-pyrimidinyl]amino}benzamide hydrochloride (1:1)
UNII-K37N7BYX3X
K37N7BYX3X
Nilotinib HCl

Biological Activity

[Description]:

Nilotinib (AMN107) hydrochlorid is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity[1][2][3].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Bcr-Abl
Signaling Pathways >> Autophagy >> Autophagy

[In Vitro]

Nilotinib hydrochlorid, selective Abl inhibitor, is designed to interact with the ATP-binding site of BCR-ABL with a higher affinity than imatinib while being significantly more potent compared with imatinib (IC50<30 nM), also maintains activity against most of the BCR-ABL point mutants that confer Imatinib resistance[1]. Nilotinib hydrochlorid demonstrates significant antitumor efficacy against GIST xenograft lines and imatinib-resistant GIST cell lines which parent cell lines GK1C and GK3C shows imatinib sensitivity with IC50 of 4.59±0.97 µM and 11.15±1.48 µM, respectively, imatinib-resistant cell lines GK1C-IR and GK3C-IR shows Imatinib resistance with IC50 values of 11.74±0.17 µM (P<0.001) and 41.37±1.07 µM (P<0.001), respectively[2].

[In Vivo]

Nilotinib hydrochlorid (oral gavage, 40 mg/kg, daily, 4 weeks) shows equivalent or higher antitumor effects in BALB/cSLc-nu/nu mice with GIST xenograft[2]. Nilotinib hydrochlorid has a significant healing effect on the macroscopic and microscopic pathologic scores and ensures considerable mucosal healing in the indomethacin-induced enterocolitis rat model while decreases the PDGFR α and β levels and apoptotic scores in the colon[3]. Animal Model: BALB/cSLc-nu/nu mice with GIST xenograft (GK1X, GK2X and GK3X)[2] Dosage: 40 mg/kg Administration: Oral gavage; daily; 4 weeks Result: Inhibited tumor growth by 69.6% in GK1X, 85.3% in GK2X and 47.5% in GK3X xenograft line.

[References]

[1]. Weisberg E, et al. Beneficial effects of combining nilotinib and imatinib in preclinical models of BCR-ABL+ leukemias. Blood. 2007 Mar 1;109(5):2112-20.

[2]. Sako H, et al. Antitumor effect of the tyrosine kinase inhibitor Nilotinib on gastrointestinal stromal tumor (GIST) and Imatinib-resistant GIST cells. PLoS One. 2014 Sep 15;9(9):e107613.

[3]. Meirson T, et al. Targeting invadopodia-mediated breast cancer metastasis by using ABL kinase inhibitors. Oncotarget. 2018 Apr 24;9(31):22158-22183.

Chemical & Physical Properties

[ Molecular Formula ]:
C28H23ClF3N7O

[ Molecular Weight ]:
565.977

[ Exact Mass ]:
565.160461

[ PSA ]:
101.11000

[ LogP ]:
7.61480

[ Storage condition ]:
-20℃

Related Compounds