CEP-40783
- Product Name
- CEP-40783
- CAS No.
- 1437321-24-8
- Chemical Name
- CEP-40783
- 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-
- CBNumber
- CB93167640
- Molecular Formula
- C31H26F2N4O6
- Formula Weight
- 588.56
- MOL File
- 1437321-24-8.mol
CEP-40783 Property
- 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)
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 25749
- Product name
- CEP-40783
- Packaging
- 1mg
- Price
- $37
- Updated
- 2024/03/01
- Product number
- 25749
- Product name
- CEP-40783
- Packaging
- 5mg
- Price
- $161
- Updated
- 2024/03/01
- Product number
- 25749
- Product name
- CEP-40783
- Packaging
- 10mg
- Price
- $283
- Updated
- 2024/03/01
- Product number
- 25749
- Product name
- CEP-40783
- Packaging
- 25mg
- Price
- $618
- Updated
- 2024/03/01
- Product number
- CS-6371
- Product name
- CEP-40783
- Purity
- 99.22%
- Packaging
- 100mg
- Price
- $650
- Updated
- 2021/12/16
CEP-40783 Chemical Properties,Usage,Production
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 |