943540-75-8 Usage
Uses
Used in Oncology:
J&J Ex-61 is used as an anticancer agent for its ability to reduce radiation-induced invasion, apoptosis, and proliferation of cancer cells in vitro. Its high selectivity for c-Met makes it a promising candidate for targeted cancer therapies.
Used in Pharmaceutical Industry:
J&J Ex-61 is used as a research compound for studying the role of c-Met in various cellular processes and its potential as a therapeutic target for cancer treatment. Its high selectivity and in vitro efficacy make it a valuable tool for drug discovery and development.
Biological Activity
jnj-38877605 is a small-molecule atp-competitive inhibitor of the catalytic activity of c-met.extensive evidence that c-met signaling is involved in the progression and spread of several cancers and an enhanced understanding of its role in disease have generated considerable interest in c-met and hgf asmajor targets in anti-cancer drug development.
in vitro
jnj-38877605 showed ~600-fold selectivity for c-met compared with a panel of ~250 diverse tyrosine and serine-threonine kinases and was found to potently inhibit hgf-stimulated and constitutively activated c-met phosphorylation in vitro [1].
in vivo
jnj-38877605 showed excellent oral bioavailability approaching 100% in all examined species. in addition, jnj-38877605 in a single dose was observed toinhibit met phosphorylation in tumor xenografts for up to16 h. inhibition of met phosphorylation was associated withdose-dependent tumor growth inhibition using a range of oral dosing regimens [2].
references
[1] pererat, l avrijssent, janssens b, et al. jnj-38877605: a selective met kinase inhibitor inducingregression of met-driven tumor models. presented at the 99th aacr annual meeting; 2008 apr 12 -16;
Check Digit Verification of cas no
The CAS Registry Mumber 943540-75-8 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,4,3,5,4 and 0 respectively; the second part has 2 digits, 7 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 943540-75:
(8*9)+(7*4)+(6*3)+(5*5)+(4*4)+(3*0)+(2*7)+(1*5)=178
178 % 10 = 8
So 943540-75-8 is a valid CAS Registry Number.
InChI:InChI=1/C19H13F2N7/c1-27-11-13(10-23-27)16-6-7-17-24-25-18(28(17)26-16)19(20,21)14-4-5-15-12(9-14)3-2-8-22-15/h2-11H,1H3
943540-75-8Relevant academic research and scientific papers
POLYMORPHIC AND HYDRATE FORMS, SALTS AND PROCESS FOR PREPARING 6-{DIFLUORO[6-(1-METHYL-1H-PYRAZOL-4-YL)[1,2,4]TRIAZOLO[4,3-B]PYRIDAZIN-3-YL]METHYL}QUINOLINE
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, (2009/01/23)
The invention relates to novel polymorphic and hydrate forms and salts of 6-{difluoro[6-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl}quinoline, to methods for their preparation, to pharmaceutical compositions comprising at least one of said polymorphic or hydrate forms or salts, and to the therapeutic and/or prophylactic use of such compositions. The invention also provides new manners for preparing said compound.
