| Name | Rociletinib |
| Description | Rociletinib (CNX-419) is an orally available small molecule, irreversible inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity. |
| Cell Research | Cells are seeded at 3,000 cells per well in growth media supplemented with 5% FBS, 2 mmol/L, L-glutamine, and 1% penicillin–streptomycin, allowed to adhere overnight, and treated with a dilution series of test compounds for 72 hours. Cell viability is determined by CellTiter-Glo, and results are represented as background-subtracted relative light units normalized to a dimethyl sulfoxide (DMSO)–treated control. Growth inhibition (GI 50) values are determined by GraphPad Prism 5.04. MK-2206 and XL-880 compounds are obtained from Selleck Chemical. CI data are generated using CalcuSyn.(Only for Reference) |
| Kinase Assay | Inhibition Kinetics Studies: Recombinant human wild-type and T790M/L858R double mutant EGFR, both Nterminal GST-tagged, are used in the assay. The Omnia continuous read assay is performed as described by the vendor. |
| In vitro | CO-1686 demonstrates significant dose-dependent tumor growth inhibition across all models of EGFR mutations, including transgenic mice expressing EGFRL858R- and EGFRL858R/T790M. |
| In vivo | CO-1686 selectively inhibits the growth of NSCLC (non-small cell lung cancer) cells expressing mutant EGFR, with a GI50 range of 7 to 32 nM, and induces apoptosis. NSCLC cell lines resistant to CO-1686 show signs of epithelial-mesenchymal transition and increased sensitivity to AKT inhibitors. In cells expressing mutant EGFR, CO-1686 inhibits p-EGFR with an IC50 range of 62 to 187 nM, while also inhibiting EGFR phosphorylation in three types of cells expressing WT (wild type) EGFR, with an IC50 of >2,000 nM. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 93 mg/mL (167.4 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | CNX 419 | AVL 301 | HER1 | Inhibitor | inhibit | CO 1686 | EGFR | ErbB-1 | Rociletinib | AVL301 | CNX419 | Epidermal growth factor receptor | CO1686 |
| Inhibitors Related | Osimertinib | Lidocaine Hydrochloride hydrate | Lapatinib | Afatinib Dimaleate | Erlotinib hydrochloride | Erlotinib | Neratinib | Chalcone | Osimertinib mesylate | Genistein | Khellin | Gefitinib |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library |
United States
