An EGFR inhibitor (IC50 = 2 nM); selective for EGFR over Abl

Icotinib – 1 mg

Brand:
Cayman
CAS:
610798-31-7
Storage:
-20
UN-No:
Non-Hazardous - /

Icotinib is an inhibitor of EGFR (IC50 = 2 nM).{57218} It is selective for EGFR over Abl, Abl2, and c-Src tyrosine kinases at 1,000 nM. Icotinib inhibits EGFR-mediated tyrosine phosphorylation in A431 human epidermoid carcinoma cells with an IC50 value of 45 nM. It inhibits the growth of PC-9 and HCC827 non-small cell lung cancer (NSCLC) cells (IC50s = 50 = 8,800 nM), which do not.{57219} It also inhibits migration of HCC827 cells when used at a concentration of 100 nM and increases apoptosis by 43.7% at 10 nM. Icotinib reduces tumor growth in a variety of mouse xenograft models when administered at doses ranging from 50 to 120 mg/kg per day.  

 

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SKU: 30093 - 1 mg Category:

Description

An EGFR inhibitor (IC50 = 2 nM); selective for EGFR over Abl, Abl2, and c-Src tyrosine kinases at 1,000 nM; inhibits EGFR-mediated tyrosine phosphorylation in A431 cells (IC50 = 45 nM); inhibits the growth of PC-9 and HCC827 NSCLC cells (IC50s = 50 = 8,800 nM), which do not; inhibits migration of HCC827 cells at 100 nM and increases apoptosis by 43.7% at 10 nM; reduces tumor growth in a variety of mouse xenograft models at 50-120 mg/kg per day

Formal name: N-(3-ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine

Synonyms:  BPI 2009H

Molecular weight: 391.4

CAS: 610798-31-7

Purity: ≥98%

Formulation: A crystalline solid

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