1185763-69-2 Usage
Description
NVP-BVU 972 is a potent and selective inhibitor of the MET kinase, a receptor tyrosine kinase that plays a crucial role in cell proliferation, survival, and migration. It is characterized by its strong inhibitory effect on MET kinase, while showing low inhibition against other kinases, including the closely related RON kinase.
Uses
Used in Pharmaceutical Industry:
NVP-BVU 972 is used as a targeted therapy for cancer treatment, particularly for tumors that overexpress the MET kinase. Its high selectivity for MET kinase makes it a promising candidate for the development of drugs to treat cancer, as it can effectively inhibit the growth and progression of cancer cells without affecting other kinases.
Used in Research Applications:
NVP-BVU 972 is also used as a research tool to study the role of MET kinase in various cellular processes, such as cell proliferation, survival, and migration. Its strong inhibitory effect on MET kinase allows researchers to investigate the specific functions and signaling pathways regulated by this kinase, providing valuable insights into the molecular mechanisms underlying cancer development and progression.
Biological Activity
nvp-bvu972 is a selective and potent inhibitor of c-met with ic50 of 14 nm. besides, nvp-bvu972 displays ic50 values more than 1000 nm in other kinases such as the most closely related kinase recepteur d'origine nantais (ron).c-met, also known as hepatocyte growth factor receptor, is a receptor tyrosine kinase that can be activated by hepatocyte growth factor/scatter factor (hgf/sf). it is a membrane protein which plays an essential role in embryonic development and wound healing.in the ebc-1, gtl-16, and mkn-45 human cancer cells, nvp-bvu972 potently inhibits the cell proliferation with ic50 values of 82, 66 and 32 nm, respectively. additionally, nvp-bvu972 treatment leads to the inhibition of the growth of the transformed mouse baf3 cells containing tpr-met kinase fusions with ic50 of 104 nm 1.in human sample, nvp-bvu972 treatment on cells expressing wild-type tpr-met resulted in a dose-dependent reduction in tpr-met phosphorylation. y1230h, d1228a, f1200i and l1195v mutations abrogate the tpr-met phosphorylation inhibition effect of nvp-bvu972 in baf3 tpr-met1.
references
1. tiedt r, degenkolbe e, furet p, et al. a drug resistance screen using a selective met inhibitor reveals a spectrum of mutations that partially overlap with activating mutations found in cancer patients. cancer research. 2011;71(15):5255-5264.
Check Digit Verification of cas no
The CAS Registry Mumber 1185763-69-2 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,1,8,5,7,6 and 3 respectively; the second part has 2 digits, 6 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 1185763-69:
(9*1)+(8*1)+(7*8)+(6*5)+(5*7)+(4*6)+(3*3)+(2*6)+(1*9)=192
192 % 10 = 2
So 1185763-69-2 is a valid CAS Registry Number.
1185763-69-2Relevant articles and documents
IMIDAZO [1,2-B] PYRIDAZINE DERIVATIVES FOR THE TREATMENT OF C-MET TYROSINE KINASE MEDIATED DISEASE
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Page/Page column 77-78, (2009/10/21)
The invention relates to compounds of formula (I) and salts thereof, formula (I) wherein the substituents are as defined in the specification, the application of a compound of formula (I) in a process for the treatment of the human or animal body, in particular with regard to C-Met tyrosine kinase mediated disease; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharamaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner; processes for the preparation of a compound of formula (I).
