LY2801653 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

LY2801653 is an orally bioavailable MET kinase inhibitor (K_i = 2 nM). It also inhibits MST1R, Axl, MNK1/2, FLT3, DDR1, and DDR2 (IC₅₀s = 11, 2, 7, 7, 0.1, and 7 nM, respectively, in a cell-based assay). It inhibits MET autophosphorylation stimulated by hepatocyte growth factor (HGF) in H460 and S114 cells (IC₅₀s = 35.2 and 59.2 nM, respectively) and inhibits growth of Ba/F3 cells transfected with MET-activating mutations (IC₅₀s = 12-248 nM). LY2801653 (0.01-10 μM) completely blocks cell scattering induced by HGF in DU145 cells. It reduces tumor growth in MET autocrine (U-87MG) and MET over-expression (H441) mouse xenograft models when administered at doses of 4 and 12 mg/kg.

Mechanism of action

LY2801653(Merestinib) inhibited phosphorylation of eIF4E in MV4-11, MM6 and AML-PT cells, blocked the cell cycle in the G0/G1 phase by decreasing the expression of cyclin A2 and cyclin B1, arrested colony formation, induced apoptosis in MV4-11 cells and exhibited antileukemic properties in vivo.

Clinical Use

Preclinical testing also has shown merestinib to inhibit several other receptor tyrosine oncokinases including MST1R, FLT3, AXL, MERTK, TEK, ROS1, and NTRK1/2/3.

LY2801653 Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

LY2801653 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
Suzhou ARTK Medchem Co., Ltd.	+8618118463618	sales1@artkmedchem.com	China	39021	58
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	33024	60
Biochempartner	0086-13720134139	candy@biochempartner.com	CHINA	965	58
career henan chemical co	+86-0371-86658258 +8613203830695	factory@coreychem.com	China	29792	58
Shaanxi Dideu Medichem Co. Ltd	+86-29-81139210 17389186172	1077@dideu.com	China	3801	58
Suzhou Ryan Pharmachem Technology Co.,Ltd.	+86-512-68780025	sales@ryanchem.com	China	169	58
TargetMol Chemicals Inc.	+1-781-999-5354; +17819995354	marketing@targetmol.com	United States	32466	58
HANGZHOU CLAP TECHNOLOGY CO.,LTD	86-571-88216897,88216896 13588875226	sales@hzclap.com	CHINA	6312	58
Zhejiang J&C Biological Technology Co.,Limited	+1-2135480471 +1-2135480471;	sales@sarms4muscle.com	China	10473	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6391	58

1206799-15-6()Verwandte Suche:

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• LY2801653
• N-(3-fluoro-4-((1-Methyl-6-(1H-pyrazol-4-yl)-1H-indazol-5-yl)oxy)phenyl)-1-(4-fluorophenyl)-6-Methyl-2-oxo-1,2-dihydropyridine-3-carboxaMide
• 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
• LY2801653(Merestinib)
• N-(3-Fluoro-4-((1-methyl-6-(1H-pyrazol-4-yl)-1H-indazol-5-yl)oxy)phenyl)-1-(4-fluorophenyl)-6-
• Merestinib(LY 2801653)
• N-[3-fluoro-4-[1-methyl-6-(1h-pyrazol-4-yl)indazol-5-yl]oxyphenyl]-1-(4-fluorophenyl)-6-methyl-2-oxopyridine-3-carboxamide
• CS-685
• MET inhibitor
• MET INHIBITOR; LY2801653; LY-2801653; LY 2801653; MERESTINIB
• 3-Pyridinecarboxamide, 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-
• NSC 32624
• NSC32624
• NSC-32624
• Merestinib, 10 mM in DMSO
• 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
• Merestinib(LY 2801653), 98%min
• Merestinib (LY2801653) ，S7014
• Merestinib
• 1206799-15-6
• C30H22F2N6O3
• API