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LY 2801653 dihydrochloride

Basic information Safety Supplier Related

LY 2801653 dihydrochloride Basic information

Product Name:
LY 2801653 dihydrochloride
Synonyms:
  • CS-1046
  • LY-2801653 DIHYDROCHLORIDE; LY 2801653 DIHYDROCHLORIDE;LY2801653
  • Merestinib(LY2801653 dihydrochloride)
  • LY 2801653 dihydrochloride
  • LY2801653 (dihydrochloride)
  • LY-2801653 dihydrochloride
  • N-[3-Fluoro-4-[[1-methyl-6-(1H-pyrazol-4-yl)-1H-indazol-5-yl]oxy]phenyl]-1-(4-fluorophenyl)-1,2-dihydro-6-methyl-2-oxo-3-pyridinecarboxamide hydrochloride (1:2)
  • LY2801653 2HCl
CAS:
1206801-37-7
MF:
C30H23ClF2N6O3
MW:
589
Mol File:
1206801-37-7.mol
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LY 2801653 dihydrochloride Chemical Properties

storage temp. 
Store at -20°C, sealed storage, away from moisture
solubility 
DMSO: ≥ 100 mg/mL (159.88 mM)
form 
Powder
color 
White to light yellow
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LY 2801653 dihydrochloride Usage And Synthesis

Uses

N-[3-Fluoro-4-[[1-methyl-6-(1H-pyrazol-4-yl)-1H-indazol-5-yl]oxyphenyl]-1-(4-fluorophenyl)-6-methyl-2-oxopyridine-3-carboxamide dihydrochloride is used as a reactant/reagent in synthetic preparation of amidophenoxyindazoles as inhibitors of c-Met.

in vivo

Merestinib (LY2801653) demonstrates anti-tumor effects in MET amplified (MKN45), MET autocrine (U-87MG, and KP4) and MET over-expressed (H441) xenograft models; and in vivo vessel normalization effects. Merestinib (LY2801653) is a type-II ATP competitive, slow-off inhibitor of MET tyrosine kinase with a pharmacodynamic residence time (Koff) of 0.00132 min-1 and t1/2 of 525 min. Merestinib (LY2801653) treatment inhibits MET phosphorylation with a composite TED50 (50 % target inhibition dose) of 1.2 mg/kg and a composite TED90 (90 % target inhibition dose) of 7.4 mg/kg[1]. Merestinib (LY2801653) (20 mg/kg) reduces TFK-1 tumor growth significantly relative to vehicle control. Merestinib (LY2801653) inhibits the growth of intra- and extrahepatic CCC xenograft tumors[2].

LY 2801653 dihydrochlorideSupplier

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