Nilotinib hydrochloride

SKU: orb1704814

Description

Nilotinib hydrochloride is an orally bioavailable Bcr-Abl tyrosine kinase inhibitor used in chronic myelogenous leukemia research. It has demonstrated activity in preclinical studies investigating neuroinflammation and cognitive deficits, showing potential in both in vitro and in vivo experimental models.

Research Area

Cardiovascular Research, Cell Biology, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 923288-95-3
• MW: 565.98
• Purity: >99.99% (May vary between batches)
• Formula: C₂₈H₂₃ClF₃N₇O
• SMILES: Cl.O=C(NC=1C=C(C=C(C1)C(F)(F)F)N2C=NC(=C2)C)C3=CC=C(C(=C3)NC=4N=CC=C(N4)C5=CN=CC=C5)C
• Target: Autophagy,Bcr-Abl
• Solubility: DMSO:90 mg/mL (159.02 mM);Ethanol:1 mg/mL (1.77 mM)

Bioactivity

• Target IC50:
  BCR-ABL:<30 nM
• 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. 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.
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• 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. 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Nilotinib Hydrochloride, AMN-107 HCl, Autophagy, BcrAbl, Bcr-Abl

Compound Identifiers

PubChem CID

16006490