[CAS NO. 1374640-70-6] Rociletinib (CO-1686)
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PRODUCTS SPECIFICATIONS [1374640-70-6]
Store
Catalog
SLK-S7284
Brand
Selleck
CAS
1374640-70-6
DESCRIPTION [1374640-70-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 555.55 |
| Molecular Formula | C27H28F3N7O3 |
| SMILES | - |
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 | 1.8000 mL | 9.0001 mL | 18.0002 mL |
| 5 mM | 0.3600 mL | 1.8000 mL | 3.6000 mL |
| 10 mM | 0.1800 mL | 0.9000 mL | 1.8000 mL |
| 50 mM | 0.0360 mL | 0.1800 mL | 0.3600 mL |
Description
Rociletinib (CO-1686, AVL-301) is an irreversible, mutant-selective inhibitor with of 21.5 nM and 303.3 nM for EGFR and EGFR in cell-free assays, respectively. Phase 2.
In vitro
CO-1686 inhibits p-EGFR with IC50 ranging from 62 to 187 nM in the mutant EGFR–expressing cells, while inhibits EGFR phosphorylation with IC50 of > 2,000 nM in the three WT EGFR–expressing cells. CO-1686 selectively inhibits growth of NSCLC cells expressing mutant EGFR with GI50 ranging from 7 to 32 nM, and induces apoptosis. CO-1686–resistant NSCLC cell lines exhibits signs of epithelial-mesenchymal transition and increased sensitivity to AKT inhibitors.
In vivo
CO-1686 causes dose-dependent and significant tumor growth inhibition in all EGFR-mutant models as well as human EGFRL858R- and EGFRL858R/T790M-expressing transgenic mice.
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