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Rociletinib

Covalent Inhibitor of EGFR (Mutant:L858R/T790M)

Structure

Information

  • EGFR (Mutant:L858R/T790M)
  • Covalent Inhibitor
  • 100 - 1000 nM

In Vitro Validations

Uniprot ID: P00533
Target Class: Kinase
Target SubClass: RTK
Potency: Ki
Potency Value: 21.5 nM L858R/T790M; 303.3 nM WT
Potency Assay: Continuous Omnia® Read Assay
PDB ID for probe-target interaction (3D structure): 5XDL,  5XDK
Target aliases:
Epidermal growth factor receptor, HER1, ERBB1, ERB ...

DOI Reference: 10.1158/1535-7163.MCT-13-0966

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Rociletinib selectivity was tested against 434 kinases in duplicate at a concentration of 0.1μM and ATP concentration of 10μM. Rociletinib inhibited 13 kinases greater than 50% with FTL3 inhibition at 94%, although IC50-apparent was only 223 nM (vs 0.5 EGFR L858R/T790M)

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SERP ratings and comments

No SERP comments found for Rociletinib