Introduction：Basic information about LY2801653 CAS 1206799-15-6, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
LY2801653 Basic information
| Product Name: | LY2801653 |
| Synonyms: | 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;Merestinib;LY2801653(Merestinib);CS-685;MET inhibitor;MET INHIBITOR; LY2801653; LY-2801653; LY 2801653; MERESTINIB |
| CAS: | 1206799-15-6 |
| MF: | C30H22F2N6O3 |
| MW: | 552.53 |
| EINECS: | 806-589-8 |
| Product Categories: | API |
| Mol File: | 1206799-15-6.mol |
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LY2801653 Chemical Properties
| Boiling point | 795.3±60.0 °C(Predicted) |
| density | 1.42±0.1 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| solubility | ≥27.65 mg/mL in DMSO; insoluble in H2O; ≥5.02 mg/mL in EtOH with gentle warming and ultrasonic |
| form | solid |
| pka | 10.83±0.70(Predicted) |
| color | White to yellow |
| InChI | InChI=1S/C30H22F2N6O3/c1-17-3-9-23(30(40)38(17)22-7-4-20(31)5-8-22)29(39)36-21-6-10-27(25(32)12-21)41-28-11-18-16-35-37(2)26(18)13-24(28)19-14-33-34-15-19/h3-16H,1-2H3,(H,33,34)(H,36,39) |
| InChIKey | QHADVLVFMKEIIP-UHFFFAOYSA-N |
| SMILES | C1(=O)N(C2=CC=C(F)C=C2)C(C)=CC=C1C(NC1=CC=C(OC2C(C3=CNN=C3)=CC3=C(C=2)C=NN3C)C(F)=C1)=O |
Safety Information
LY2801653 Usage And Synthesis
| Description | LY2801653 is an orally bioavailable MET kinase inhibitor (Ki = 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. |
| Description | MET is a tyrosine kinase that leads to downstream activation of several pathways including RAS and MAPK.?As a result, it is quite possible that MET inhibition can be active in RAS mutant tumors and maybe associated with EGFR resistance in NSCLC.?Two MET inhibitors, tivantinib and onartuzumab, have been examined in KRAS mutant NSCLC with others in clinical trials at this time. |
| Uses | LY2801653(Merestinib), a c-MET inhibitor developed by Lilly, has shown promising therapeutic effects in many solid tumors by targeting c-MET/HGFR and is used in clinical trials to treat a variety of oncolytic indications. |
| 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. |
| target | c-MET |
| references | [1] yan s b et al. , ly2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against met, mst1r, and other oncoproteins, and displays anti-tumor activities in mouse xenograft models. invest new drugs. 2012, 31: 833-844. |
LY2801653 Preparation Products And Raw materials
