| Name | Nilotinib hydrochloride |
| 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. |
| 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] |
| Storage | Store at low temperature | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 90 mg/mL (159.02 mM), Sonication is recommended.
Ethanol : 1 mg/mL (1.77 mM), Sonication is recommended.
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| Keywords | Nilotinib Hydrochloride | Bcr-Abl | BcrAbl | Autophagy |
| Inhibitors Related | Stavudine | Aceglutamide | Hemin | Tamoxifen | Cysteamine hydrochloride | Guanidine hydrochloride | Hydroxychloroquine | Enzalutamide | Paeonol | Naringin | Alginic acid | Sildenafil citrate |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Anti-Cancer Approved Drug Library | FDA-Approved Kinase Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library |
United States
