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Rociletinib hydrobromide is an orally delivered inhibitor of the mutant form of EGFR kinase (Kis: 21.5 nM and 303.3 nM for EGFR L858R/T790M and EGFR WT).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $39 | 7-10 days | 7-10 days | |
| 10 mg | $67 | 7-10 days | 7-10 days | |
| 1 mL x 10 mM (in DMSO) | $55 | 7-10 days | 7-10 days |
| Description | Rociletinib hydrobromide is an orally delivered inhibitor of the mutant form of EGFR kinase (Kis: 21.5 nM and 303.3 nM for EGFR L858R/T790M and EGFR WT). |
| Targets&IC50 | EGFR (L858R/T790M):21.5 nM (ki), EGFR (T790M):303.3 nM (ki) |
| In vitro | Rociletinib resistant NSCLC cell lines are sensitive to AKT inhibition. Rociletinib selectively inhibits the growth of NSCLC cells expressing mutant EGFR and induces apoptosis. Rociletinib (0.1 μM) inhibits EGFR potently and irreversibly. It inhibits more than 50% of 23 targets. |
| In vivo | Rociletinib (50 mg/kg bid, p.o.) shows anti-tumor activity in human EGFR-L858R and EGFR-L858R-T790M expressing transgenic mice. Rociletinib (100 mg/kg/day, p.o.) displays anti-tumor activity in NSCLC EGFR mutant xenograft models. |
| Synonyms | CO-1686 (hydrobromide), CNX-419 hydrobromide, AVL-301 hydrobromide |
| Molecular Weight | 636.46 |
| Formula | C27H29BrF3N7O3 |
| Cas No. | 1446700-26-0 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 59 mg/mL (92.7 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2.5 mg/mL (3.93 mM), Sonication is recommeded. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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