www.mayflowerbio.com
Sales & Support: 314-485-5210

*

Osimertinib

Supplier:
Catalogue number:
10-5036-02
Size:
50 mg
Product is available in:
  • USA
  • Canada
$150.00 Shipping is calculated in checkout

Mutant EGFR kinase inhibitor / Osimertinib is a potent, selective, irreversible inhibitor of mutant EFGR tyrosine kinase.1 Osimertinib inhibits phosphorylation of EGFR in T790M-mutant cell lines (IC50 <15 nM) but was less potent at inhibition of EGFR phosphorylation in wild-type cells (IC50s in the range of 480 to 1,865 nM). It produces sustained tumor regression in EGFR-mutant tumor xenograft and transgenic rodent models.2 Tumor cells develop resistance to osimertinib but combination treatment with an IL-6 antibody reverses resistance to a certain extent.3 In clinical use for treatment of non-small cell lung cancer.4

Product Type:

Biochemicals & reagents

CAS Number:

1421373-65-0

Alternative Names:

AZD-9291

Reference:

1 Finlay et al. (2014), Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor; J. Med. Chem., 57 8249 2 Cross et al. (2014), AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer; Cancer Discov., 4 1046 3 Tan et al. (2024), Evaluation of drug resistance for EGFR-TKIs in lung cancer via multicellular lung-on-a-chip; Eur. J. Pharm. Sci., 199 106805 4 Patel et al. (2017); Recent updates on third generation EGFR inhibitors and emergence of fourth generation EGFR inhibitors to combat C797S resistance; J. Med. Chem., 142 32

Storage Temperature:

-20°C

Additional Information:

TARGET: Kinase -- PATHWAY: EGF -- DISEASE AREA: Cancer