923288-90-8 Usage
Description
Nilotinib hcl monohydrate, also known as Nilotinib Monohydrochloride Monohydrate, is a pharmaceutical compound with potential applications in the treatment of chronic myelogenous leukemia and as a research product for COVID-19 related studies.
Used in Pharmaceutical Industry:
Nilotinib hcl monohydrate is used as an antineoplastic agent for the treatment of chronic myelogenous leukemia, a type of blood cancer. It works by inhibiting the activity of the BCR-ABL tyrosine kinase, which is a key driver of the disease.
Used in COVID-19 Research:
Nilotinib hcl monohydrate is used as a research product in the study of COVID-19, the disease caused by the SARS-CoV-2 virus. Its potential role in this context is still under investigation, but it may offer insights into the development of new treatments or therapies for this global health challenge.
Clinical Use
Nilotinib hydrochloride monohydrate was approved by FDA in 2007 for the treatment of chronic and accelerated phase Ph chromosome-positive CML adult patients which have developed resistance or intolerance to prior therapy that included imatinib. In 2012, apart from these previous indications, nilotinib hydrochloride monohydrate has also been indicated for the treatment of newly diagnosed adult patients with Ph chromosome-positive CML in chronic phase.
Mechanism of action
Tasigna (nilotinib hydrochloride monohydrate) is an orally available signal transduction inhibitor of the Bcr-Abl kinase, c-kit and Platelet Derived Growth Factor (PDGF). Nilotinib binds to and stabilizes the inactive conformation of the kinase domain of Abl protein. In vitro, nilotinib inhibited Bcr-Abl mediated proliferation of murine leukemic cell lines and human cell lines derived from Ph+ CML patients. In vivo, nilotinib reduced the tumor size in a murine Bcr-Abl xenograft model.
Side effects
a headache, fatigue, gastrointestinal problems such as nausea, vomiting, diarrhea and constipation, muscle and joint pain, rash and other skin conditions, flu-like symptoms, and reduced blood cell count. Less typical side effects are those of the cardiovascular system, such as hypertension (high blood pressure), various types of arrhythmia, and prolonged QT interval. Interaction of nilotinib with OATP1B1 and OATP1B3 may alter its hepatic disposition and can lead to transporter mediated drug-drug interactions.
in vitro
In vitro, nilotinib inhibited Bcr-Abl mediated proliferation of murine leukemic cell lines and human cell lines derived from Ph+ CML patients. Under the conditions of the assays, nilotinib was able to overcome imatinib resistance resulting from Bcr-Abl kinase mutations, in 32 out of 33 mutations tested. In vivo, nilotinib reduced the tumor size in a murine Bcr-Abl xenograft model. Nilotinib inhibited the autophosphorylation of the following kinases at IC50 values as indicated: Bcr-Abl (20-60 nM), PDGFR (69 nM) and c-Kit (210 nM). Nilotinib is currently being trialed in people with Parkinson's disease, as it appears to be able to halt progression of the disease and even improve their symptoms.
Check Digit Verification of cas no
The CAS Registry Mumber 923288-90-8 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,2,3,2,8 and 8 respectively; the second part has 2 digits, 9 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 923288-90:
(8*9)+(7*2)+(6*3)+(5*2)+(4*8)+(3*8)+(2*9)+(1*0)=188
188 % 10 = 8
So 923288-90-8 is a valid CAS Registry Number.
923288-90-8Relevant articles and documents
CRYSTALLINE FORMS OF 4-METHYL-N-[3-(4-METHYL-IMIDAZOL-1-YL)-5-TRIFLUOROMETHYL-PHENYL]-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-BENZAMIDE
-
Page/Page column 28, (2008/06/13)
Crystalline forms of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide free base and salts thereof are prepared by various processes.