Product Name

Rociletinib

General description

Rociletinib 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.

Synonym

CO-1686, AVL-301

Purity

≥98.0%(HPLC)

CAS Number

1374640-70-6

Formula

C²⁷H²⁸F³N⁷O³

Molecular Weight

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

solid

Solubility(25℃)

DMSO

≥50mg/mL

Ethanol

Insoluble

Water

Insoluble

l  Biological Information

Biochem/Physiol  Actions

Rociletinib is an orally available small molecule, irreversible inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Rociletinib binds to and inhibits mutant forms of EGFR, including T790M, thereby leading to cell death of resistant tumor cells. Compared to other EGFR inhibitors, CO-1686 inhibits T790M, a secondary acquired resistance mutation, as well as other mutant EGFRs and may have therapeutic benefits in tumors with T790M-mediated resistance to other EGFR tyrosine kinase inhibitors. This agent shows minimal activity against wild-type EGFR, hence does not cause certain dose-limiting toxicities.

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.

l  Storage

Storage temp.

-20℃

l  Precautions and Disclaimer

This product is for R&D use only, not for drug, household, or other uses.

l  References

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov