An inhibitor of EGFRs (IC50s = 3.2

Poziotinib – 25 mg

Brand:
Cayman
CAS:
1092364-38-9
Storage:
-20
UN-No:
Non-Hazardous - /

Poziotinib is a potent inhibitor of EGFR family kinases with IC50 values of 3.2, 5.3, 23.5, 4.2, and 2.2 nM for wild-type EGFR, HER2, HER4, EGFRT790M, and EGFRL858R/T790M, respectively.{38157} It has greater than 100- to 1,000-fold selectivity for EGFR kinases over 30 other tested kinases in vitro. Poziotinib inhibits growth of wild-type and mutant EGFR kinase-dependent lung, breast, and gastric cancer cell lines (GI50s = 0.6-5.7 nM) and inhibits EGFR phosphorylation and induces apoptosis in vitro. In vivo, poziotinib reduces tumor size in an HCC827 non-small cell lung cancer mouse xenograft model. Formulations containing poziotinib are under investigation in clinical trials for the treatment of EGFR-mutant lung adenocarcinoma.{38158}  

 

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Description

An inhibitor of EGFRs (IC50s = 3.2, 5.3, 23.5, 4.2, and 2.2 nM for wild-type EGFR, HER2, HER4, EGFRT790M, and EGFRL858R/T790M, respectively); has greater than 100- to 1,000-fold selectivity for EGFR kinases in vitro over 30 other kinases; inhibits growth of wild-type and mutant EGFR kinase-dependent lung, breast, and gastric cancer cell lines (GI50s = 0.6-5.7 nM); inhibits EGFR phosphorylation and induces apoptosis in vitro; reduces tumor size in an HCC827 non-small cell lung cancer mouse xenograft model,

Formal name: 1-[4-[[4-[(3,4-dichloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]oxy]-1-piperidinyl]-2-propen-1-one

Synonyms:  HM781-36B

Molecular weight: 491.3

CAS: 1092364-38-9

Purity: ≥95%

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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