An irreversible inhibitor of mutant forms of EGFR including T790M (Ki = 21.5 nM) with minimal activity at the wild-type EGFR (Ki = 303.3 nM); inhibits the proliferation of NSCLC cells expressing mutant EGFR (GI50s = 7-32 nM) and demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft and transgenic models

CO-1686 – 1 mg

Brand:
Cayman
CAS:
1374640-70-6
Storage:
-20
UN-No:
Non-Hazardous - /

CO-1686 is an irreversible kinase inhibitor that specifically targets mutant forms of the epidermal growth factor receptor (EGFR) including T790M (Ki = 21.5 nM) with significantly reduced activity at the wild-type form of the receptor (Ki = 303.3 nM).{27821} CO-1686 has been shown to inhibit the proliferation of non-small cell lung cancer (NSCLC) cells expressing mutant EGFR with GI50 values ranging from 7-32 nM in vitro, inducing apoptosis.{27821} It also demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft and transgenic models dosed orally at 100 mg/kg/day.{27821}  

 

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Description

An irreversible inhibitor of mutant forms of EGFR including T790M (Ki = 21.5 nM) with minimal activity at the wild-type EGFR (Ki = 303.3 nM); inhibits the proliferation of NSCLC cells expressing mutant EGFR (GI50s = 7-32 nM) and demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft and transgenic models

Formal name: N-[3-[[2-[[4-(4-acetyl-1-piperazinyl)-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]-2-propenamide

Synonyms:  AVL-301

Molecular weight: 555.6

CAS: 1374640-70-6

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 Death|Apoptosis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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