| CAS NO: | 1437321-24-8 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 588.56 |
|---|---|
| Formula | C31H26F2N4O6 |
| CAS No. | 1437321-24-8 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 10 mg/mL (16.99 mM) |
| Water: <1 mg/mL | |
| Ethanol: 2 mg/mL (3.39 mM) | |
| 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 |
| Synonyms | CEP-40783; CEP40783; CEP 40783; RXDX-106; RXDX 106; RXDX106 |
| In Vitro | In vitro activity: 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. Kinase Assay: RXDX-106 (also known as CEP-40783) is an highly orally-available, nanomolar potent and highly kinase-selective Type II inhibitor of AXL and c-Met with IC50 values of 7 nM and 12 nM, respectively. It displayed low nanomolar biochemical activity and slow (T1/2>120 min) inhibitor off-rate in peptide phosphorylation assays and in vitro kinase binding assays, respectively. Cell Assay:3T3 cells expressing Tyro3, Axl, or Mer are incubated with vehicle alone or RXDX-106 for 30 minutes, and receptor phosphorylation is monitored. |
|---|---|
| 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. |
| Animal model | SCID Beige mice |
| Formulation & Dosage | 30 mg/kg; p.o. |
| References | /13_Supplement/4191 |
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