| Identification | Back Directory | [Name]
CEP-40783 | [CAS]
1437321-24-8 | [Synonyms]
CS-2528
RXDX-106
CEP-40783
CEP-40783(RXDX-106)
RXDX-106(CEP-40783)
CEP 40783; CEP40783; RXDX-106
3-(4-fluorophenyl)-1-isopropyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid [4-(6,7-dimethoxyquinolin-4-yloxy)-3-fluorophenyl]amide
5-Pyrimidinecarboxamide, N-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]-3-fluorophenyl]-3-(4-fluorophenyl)-1,2,3,4-tetrahydro-1-(1-methylethyl)-2,4-dioxo- | [Molecular Formula]
C31H26F2N4O6 | [MDL Number]
MFCD28502441 | [MOL File]
1437321-24-8.mol | [Molecular Weight]
588.56 |
| Chemical Properties | Back Directory | [density ]
1.394±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF:20.0(Max Conc. mg/mL);33.89(Max Conc. mM)
DMF:PBS (pH 7.2) (1:2):0.3(Max Conc. mg/mL);0.51(Max Conc. mM)
DMSO:6.04(Max Conc. mg/mL);10.26(Max Conc. mM)
Ethanol:2.0(Max Conc. mg/mL);3.4(Max Conc. mM) | [form ]
A crystalline solid | [pka]
10.42±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
CEP-40783 is a potent, selective and orally potent inhibitor of axl and c-Met with IC50 values of 7nM and 12nM, respectively. | [Biological Activity]
RXDX-106 (CEP-40783) is an orally available, potent, and selective inhibitor of TAM (TYRO3, AXL, MER)/Met (c-Met), with low levels in peptide phosphorylation assays. Nanomolar biochemical activity; slow dissociation rate (T1/2 >120 min) in in vitro kinase binding assays. | [in vitro]
CEP-40783 inhibited TAM and c-MET phosphorylation, accompanied by a decrease in downstream MAPK and PI3K signaling and cellular activity. In TAM-expressing cells, sub-nanomolar concentrations of RXDX-106 completely inhibited cell proliferation and cell viability. | [in vivo]
CEP-40783 inhibits tumors with activating TAM gene fusions and affects the TAM-expressing tumor microenvironment, resulting in an overall anticancer environment. | [target]
| Target | Value | Axl
(Cell-free assay) | 7 nM | c-Met
(Cell-free assay) | 12 nM | Tyro3
(Cell-free assay) | 19 nM | MER
(Cell-free assay) | 29 nM | Tyro3
(Cell-free assay) | 29 nM |
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Tags:1437321-24-8
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