Rociletinib (CO-1686, AVL-301)
Catalog No.S7284 Synonyms: CNX-419
Molecular Weight(MW): 555.55
Rociletinib (CO-1686, AVL-301) is an irreversible, mutant-selective EGFR inhibitor with Ki of 21.5 nM and 303.3 nM for EGFRL858R/T790M and EGFRWT in cell-free assays, respectively. Phase 2.
Cited by 13 Publications
5 Customer Reviews
Immunohistochemical studies reveal the tumor cells to be negative for chromogranin and synaptophysin pre-rociletinib and positive for both neuroendocrine markers in the post-rociletinib liver biopsy. The results, in conjunction with the morphology, are consistent with the diagnosis of small cell carcinoma in the rociletinib-resistant specimen. H&E, hematoxylin and eosin.
Cancer Discov, 2015, 5(7): 713-22. Rociletinib (CO-1686, AVL-301) purchased from Selleck.
Inhibition of the phosphorylation of EGFR and downstream proteins by EGFR-TKIs in BaF3 cells harboring EGFR mutations. The results of immunoblotting for Ba/F3 cells with EGFR exon 19 deletion, L858R, exon 19 deletion+T790M, and L858R+T790M are shown. The cells were treated with the indicated concentrations of EGFR-TKIs for 4 h. Erlotinib, afatinib, osimertinib, and rociletinib were used as EGFR-TKIs. pEGFR, pAKT, and pERK indicate the phosphorylated form of EGFR, AKT, and ERK, respectively. Actin was used as a loading control.
Oncotarget, 2015, 6(36):38789-803. . Rociletinib (CO-1686, AVL-301) purchased from Selleck.
Purity & Quality Control
Choose Selective EGFR Inhibitors
|Description||Rociletinib (CO-1686, AVL-301) is an irreversible, mutant-selective EGFR inhibitor with Ki of 21.5 nM and 303.3 nM for EGFRL858R/T790M and EGFRWT in cell-free assays, respectively. Phase 2.|
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. |
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||DMSO||100 mg/mL (180.0 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Molecular Weight Calculator
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02630186||Terminated||Drug: Rociletinib|Drug: MPDL3280A||Non-small Cell Lung Cancer||Clovis Oncology Inc.|Genentech Inc.||February 24 2016||Phase 1|Phase 2|
|NCT02580708||Terminated||Drug: Rociletinib|Drug: Trametinib||Non-small Cell Lung Cancer||Clovis Oncology Inc.|Novartis Pharmaceuticals||September 30 2015||Phase 1|Phase 2|
|NCT02147990||Terminated||Drug: Rociletinib||Non-small Cell Lung Cancer||Clovis Oncology Inc.||June 16 2014||Phase 2|
|NCT01526928||Completed||Drug: Rociletinib||Locally Advanced or Metastatic Non Small Cell Lung Cancer||Clovis Oncology Inc.||March 27 2012||Phase 1|Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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