[CAS NO. 1437321-24-8] RXDX-106 (CEP-40783)
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PRODUCTS SPECIFICATIONS [1437321-24-8]
Catalog
SLK-S8570
Brand
Selleck
CAS
1437321-24-8
DESCRIPTION [1437321-24-8]
Overview
| MDL | MFCD28502441 |
|---|---|
| Molecular Weight | 588.56 |
| Molecular Formula | C31H26F2N4O6 |
| SMILES | O=C(C1=CN(C(C)C)C(N(C2=CC=C(F)C=C2)C1=O)=O)NC3=CC=C(OC4=CC=NC5=CC(OC)=C(OC)C=C45)C(F)=C3 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6991 mL | 8.4953 mL | 16.9906 mL |
| 5 mM | 0.3398 mL | 1.6991 mL | 3.3981 mL |
| 10 mM | 0.1699 mL | 0.8495 mL | 1.6991 mL |
| 50 mM | - | - | - |
Description
RXDX-106 (CEP-40783) is an orally-available, potent and selective inhibitor displaying low nanomolar biochemical activity and slow (T1/2 >120 min) inhibitor off-rate in peptide phosphorylation assays and in vitro kinase binding assays, respectively.
Targets
In vitro
RXDX-106 inhibits TAM and c-MET phosphorylation in vitro. This inhibition of TAM and c-MET activation in vitro is accompanied by a decrease in downstream MAPK and PI3K signaling and cell viability. It completely inhibits cellular proliferation and viability at sub-nanomolar concentrations in TAM-expressing cells.
In vivo
RXDX-106 could inhibit tumors harboring activating TAM gene fusions and affect the TAM-expressing tumor microenvironment to result in a global anti-cancer environment.
References
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