Osimertinib, Mutant EGFR kinase inhibitor

Product Details

Formal Name: N-[2-[[2-(Dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide

Alternate Names: AZD-9291

Molecular Formula: C₂₈H₃₃N₇O₂

Formula Weight: 499.6

CAS Number: 1421373-65-0

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (up to 40 mg/ml)

Storage: -20°C

Stability: ≥ 2 years.

Applications

Mutant EGFR kinase inhibitor

Functions

A potent, selective, irreversible inhibitor of mutant EFGR tyrosine kinase. 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. Tumor cells develop resistance to osimertinib but combination treatment with an IL-6 antibody reverses resistance to a certain extent. In clinical use for treatment of non-small cell lung cancer.

Application Procedures

First dissolved in DMSO (40 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)