An irreversible inhibitor of EGFR sensitizing and T790M resistance mutations (IC50s = 15-17 nM) while sparing the wild-type EGFR (IC50 = 480 nM); inhibits tumor growth in a xenograft mouse model at oral doses of 5-10 mg/kg

AZD 9291 – 50 mg

Brand:
Cayman
CAS:
1421373-65-0
Storage:
-20
UN-No:
Non-Hazardous - /

AZD 9291 is an irreversible inhibitor of epidermal growth factor receptor (EGFR) sensitizing and T790M resistance mutations (IC50s = 15-17 nM) while sparing the wild-type form of the receptor (IC50 = 480 nM).{27820} It binds the related IGF1R and hERG receptors with significantly reduced potency (IC50s = 2.9 and 16.2 µM, respectively).{27820} AZD 9291 has been shown to inhibit tumor growth in a xenograft mouse model at oral doses of 5-10 mg/kg and has been tested clinically in patients with advanced EGFR mutant non-small-cell lung cancer.{27820}  

 

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Description

An irreversible inhibitor of EGFR sensitizing and T790M resistance mutations (IC50s = 15-17 nM) while sparing the wild-type EGFR (IC50 = 480 nM); inhibits tumor growth in a xenograft mouse model at oral doses of 5-10 mg/kg

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

Synonyms: 

Molecular weight: 499.6

CAS: 1421373-65-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|EGFR/ErbB/HER Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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