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CO-1686 (also know as AVL-301) is an orally available small molecule, irreversible inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Rociletinib (CO-1686) selectively inhibits proliferation in the mutant-EGFR NSCLC cells with GI50 ranging from 7 to 32 nM, and induces apoptosis. In NSCLC cells with acquired resistance to CO-1686 in vitro, there was no evidence of additional mutations or amplification of the EGFR gene, but resistant cells exhibited signs of epithelial-mesenchymal transition and demonstrated increased sensitivity to AKT inhibitors. In vivo, Rociletinib (CO-1686) caused dose-dependent and significant tumor growth inhibition in all EGFR-mutant models as well as human EGFRL858R- and EGFRL858R/T790M-expressing transgenic mice. Rociletinib (CO-1686) is approximately 22-fold selective over WT EGFR (kinactt/Ki = (1.12 ± 0.14) x 104 M-1s-1).
| Cell Experiment | |
|---|---|
| Cell lines | HCC827 and HCC827-EPR cells |
| Preparation method | Cell signaling analysis of HCC827 and HCC827-EPR HCC827 and HCC827-EPR cells were seeded at 1.5×10^6 cells per 10 cm^2 dish in RPMI 1640, 10 % FBS, 2 mM L-glutamine, and 1% P/S and allowed to adhere overnight. Cells were treated with DMSO, 2 μM CO-1686, or 2 μM erlotinib for 72 hours and lysed. Lysis buffer contained 1X phenylmethanesulfonyl fluoride, 1X cell extraction buffer, 1X protease inhibitor cocktail (AbMole, M5293), 1X phosphatase inhibitor cocktails I and II. Total protein concentration was determined using a standard Bradford and measured on a NanoDrop 2000 spectrophotometer. Western blotting was performed on cell lysates normalized to 25 μg total protein in loading buffer. Normalized lysates were run on SDS/PAGE and transferred to a nitrocellulose membrane. The membrane was incubated in Qentix signal enhancement solution, blocked, and incubated overnight at 4°C with primary antibodies (1:1000) from Cell Signaling. Membranes were washed, incubated with IRDye secondary antibodies, washed again, and imaged on an Odyssey Fc. |
| Concentrations | 2µM |
| Incubation time | 72h |
| Animal Experiment | |
|---|---|
| Animal models | EGFR-L858R and EGFR-L858R-T790M;CCSP-rtTA transgenic mouse models |
| Formulation | resuspended in warmed DMSO:Solutol HS15: PBS (5:15:80; v:v:v) |
| Dosages | 50 mg/kg BID |
| Administration | oral gavage |
| Molecular Weight | 555.55 |
| Formula | C27H28F3N7O3 |
| CAS Number | 1374640-70-6 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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| Sapitinib (AZD8931)
AZD8931 (Sapitinib) is an equipotent, reversible inhibitor of Signaling by EGFR, ERBB2 (HER2), and ERBB3 with IC50 of 4, 3, 4 nM respectively. |
| Afatinib
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| CP-724714
CP-724714 is a potent and selective orally active HER-2 tyrosine kinase inhibitor, IC50 = 3 nM. |
| Erlotinib Hydrochloride
Erlotinib is an inhibitor of human EGFR tyrosine kinase (IC50 = 2 nM) and decreases EGFR autophosphorylation in tumor cells (IC50 = 20 nM). |
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