J&J Ex-61

J&J Ex-61
  • CAS No.:943540-75-8

Important Notice

  1. This product is a chemical product/pharmaceutical intermediate. It is not a drug, an active pharmaceutical ingredient (API), or a pharmaceutical-grade material. It has not been granted a drug approval number or a Chemical Drug Substance Approval Notice, has not passed drug-related review and approval, and is not manufactured, tested, or released in accordance with pharmaceutical GMP.
  2. This product is intended solely for non-clinical research, process development, quality studies, further chemical processing, or chemical synthesis. It must not be used in drug-product manufacturing, clinical trials, clinical diagnosis, or administration to humans or animals, or be sold, used as an input, submitted for regulatory filing, or released as an API or pharmaceutical material.
  3. The purchaser must not use this product, or supply it to another party, for personal consumption, sports or fitness, weight loss, health supplements, food, or animal feed.
Other grades of this product :
J&J Ex-61 Basic information
Product Name:J&J Ex-61
Synonyms:J&J Ex-61;Quinoline, 6-[difluoro[6-(1-methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]methyl]-;6-[Difluoro[6-(1-methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]methyl]quinoline;6-(Difluoro(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]-triazolo[4,3-b]pyridazin-3-yl)methyl)quinolin;JNJ-38877605;JNJ-33877605;6-[Difluoro[6-(1-methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]methyl]quinoline JNJ 38877605;JNJ 38877605 6-[Difluoro[6-(1-methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]methyl]quinoline
CAS:943540-75-8
MF:C19H13F2N7
MW:377.35
EINECS:
Product Categories:Inhibitors
Mol File:943540-75-8.mol
J&J Ex-61 Chemical Properties
density 1.50
solubility insoluble in H2O; ≥18.85 mg/mL in DMSO; ≥3.25 mg/mL in EtOH with ultrasonic
CAS DataBase Reference943540-75-8
Safety Information
MSDS Information
J&J Ex-61 Usage And Synthesis
UsesJNJ-38877605 is a potent inhibitor of c-Met catalytic activity. Selective over other tyrosine and serine-threonine kinases (600-fold selectivity). Ability to block constitutive or HGF-stimulated phosphorylation of c-Met demonstrated in vitro. JNJ 38877605 reduces radiation-induced invasion, apoptosis and proliferation of cancer cells in vitro.
Biological Activityjnj-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 vitrojnj-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 vivojnj-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;
J&J Ex-61 Preparation Products And Raw materials

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