Nilotinib hydrochloride anhydrous

Modify Date: 2024-01-19 14:16:09

Nilotinib hydrochloride anhydrous Structure
Nilotinib hydrochloride anhydrous structure
Common Name Nilotinib hydrochloride anhydrous
CAS Number 923288-95-3 Molecular Weight 565.977
Density N/A Boiling Point N/A
Molecular Formula C28H23ClF3N7O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Nilotinib hydrochloride anhydrous


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

 Names

Name 4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide,hydrochloride
Synonym More Synonyms

 Nilotinib hydrochloride anhydrous Biological Activity

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

 Synonyms

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
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