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Nilotinib hydrochloride

Catalog No. T22378   CAS 923288-95-3
Synonyms: AMN-107 HCl

Nilotinib hydrochloride(AMN-107 HCl) is an orally available Bcr-Abl tyrosine kinase inhibitor with antitumor activity for modulation of neuroinflammation and cognitive deficits, and may be used in studies of chronic myelogenous leukemia.

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Nilotinib hydrochloride Chemical Structure
Nilotinib hydrochloride, CAS 923288-95-3
Pack Size Availability Price/USD Quantity
5 mg In stock $ 40.00
10 mg In stock $ 57.00
25 mg In stock $ 94.00
50 mg In stock $ 138.00
100 mg In stock $ 209.00
500 mg In stock $ 593.00
1 mL * 10 mM (in DMSO) In stock $ 96.00
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Purity: 100%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Nilotinib hydrochloride(AMN-107 HCl) is an orally available Bcr-Abl tyrosine kinase inhibitor with antitumor activity for modulation of neuroinflammation and cognitive deficits, and may be used in studies of chronic myelogenous leukemia.
Targets&IC50 BCR-ABL:<30 nM
In vitro Nilotinib hydrochloride (AMN107 hydrochloride) is a selective Abl inhibitor designed to interact with the ATP binding site of BCR-ABL with higher affinity than imatinib while being more potent than imatinib (IC50<30 nM ), also retains activity against most BCR-ABL point mutants that confer resistance to imatinib.[1]
Nilotinib hydrochloride showed significant anti-tumor efficacy against GIST xenograft cell lines and imatinib-resistant GIST cell lines, among which the parental cell lines GK1C and GK3C showed imatinib sensitivity with IC50 of 4.59±0.97 μM and 11.15±1.48 μM, respectively.[2]
In vivo Nilotinib hydrochloride (AMN107 hydrochloride) (40 mg/kg; oral gavage; daily; for 4 weeks; BALB/cSLc-nu/nu mice with GIST xenograft) demonstrated equivalent or superior antitumor effects in BALB/cSLc-nu/nu mice with GIST xenografts. Nilotinib hydrochloride Inhibited tumor growth by 69.6% in GK1X, 85.3% in GK2X, and 47.5% in GK3X xenograft line.[2]
Nilotinib hydrochloride exerts significant healing effects on macroscopic and microscopic pathology scores in a rat model of indomethacin-induced enterocolitis and ensures considerable mucosal healing while reducing PDGFR alpha and beta levels and apoptosis in the colon Rating.[3]
Synonyms AMN-107 HCl
Molecular Weight 565.98
Formula C28H23ClF3N7O
CAS No. 923288-95-3

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90 mg/ml (159.02 mM)

Ethanol: 1 mg/ml (1.77 mM)

TargetMolReferences and Literature

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. Dervis Hakim G, et al. Mucosal healing effect of nilotinib in indomethacin-induced enterocolitis: A rat model. World J Gastroenterol. 2015 Nov 28;21(44):12576-85.

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Kinase Inhibitor Library FDA-Approved Kinase Inhibitor Library EMA Approved Drug Library Approved Drug Library Autophagy Compound Library Bioactive Compounds Library Max Bioactive Compound Library FDA-Approved & Pharmacopeia Drug Library

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Keywords

Nilotinib hydrochloride 923288-95-3 Angiogenesis Autophagy Cytoskeletal Signaling Tyrosine Kinase/Adaptors Bcr-Abl Nilotinib Hydrochloride AMN-107 HCl inhibitor inhibit

 

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