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;N-(4-((6,7-Dimethoxyquinolin-4-yl)oxy)-3-fluorophenyl)-3-(4-fluorophenyl)-1-isopropyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide;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
- Molecular Weight:
- 588.56
- MDL Number:
- MFCD28502441
- MOL File:
- 1437321-24-8.mol
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 |
FDA UNII | 1969ZJE05Q |
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS07 |
|||||||||
---|---|---|---|---|---|---|---|---|---|---|
Signal word | Warning | |||||||||
Hazard statements | H302 | |||||||||
Precautionary statements | P280-P305+P351+P338 | |||||||||
NFPA 704 |
|
CEP-40783 price More Price(14)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Cayman Chemical | 25749 | CEP-40783 | 1437321-24-8 | 1mg | $37 | 2024-03-01 | Buy |
Cayman Chemical | 25749 | CEP-40783 | 1437321-24-8 | 5mg | $161 | 2024-03-01 | Buy |
Cayman Chemical | 25749 | CEP-40783 | 1437321-24-8 | 10mg | $283 | 2024-03-01 | Buy |
Cayman Chemical | 25749 | CEP-40783 | 1437321-24-8 | 25mg | $618 | 2024-03-01 | Buy |
ChemScene | CS-6371 | CEP-40783 99.22% | 1437321-24-8 | 100mg | $650 | 2021-12-16 | Buy |
CEP-40783 Chemical Properties,Uses,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 | tr>
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32820 | 60 |
career henan chemical co | +86-0371-86658258 +8613203830695 | factory@coreychem.com | China | 29815 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32024 | 58 |
Baoji Guokang Healthchem co.,ltd | +8615604608665 15604608665 | dominicguo@gk-bio.com | CHINA | 9414 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
TargetMol Chemicals Inc. | support@targetmol.com | United States | 38463 | 58 | |
LEAPCHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 43340 | 58 |
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 57505 | 58 |
Suzhou ARTK Medchem Co., Ltd. | +86-512-68323658 +86-18168183658 | sales1@artkmedchem.com | China | 39004 | 58 |
Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131957 | 58 |