Drug & Cancer & Variant
Search content: Drug = A66
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Gene Variant Type Tumor Drug Drug level Reference More
ERBB2 AMP CNA Breast Cancer A66 V 1
Evidence region


Patient Criteria

Her2-receptor Positive


Pharmacologic (A66; p110alpha specific inhibitor) or genetic (cre-mediated knockout) ablation of the p110alpha PI3K isoform reduced tumor growth and tumor formation, respectively, in athymic mice transplanted with cells transduced by MMTV-NeuT (mammary specific overexpression of HER2 that effectively induces tumors). A66 treatment of cells from MMTV-NeuT mouse tumors resulted in decreased lipid kinase activity and phospho Akt levels.

Gene name


Full name

erb-b2 receptor tyrosine kinase 2

Gene type



This gene encodes a member of the epidermal growth factor (EGF) receptor family of receptor tyrosine kinases. This protein has no ligand binding domain of its own and therefore cannot bind growth factors. However, it does bind tightly to other ligand-bound EGF receptor family members to form a heterodimer, stabilizing ligand binding and enhancing kinase-mediated activation of downstream signalling pathways, such as those involving mitogen-activated protein kinase and phosphatidylinositol-3 kinase. Allelic variations at amino acid positions 654 and 655 of isoform a (positions 624 and 625 of isoform b) have been reported, with the most common allele, Ile654/Ile655, shown here. Amplification and/or overexpression of this gene has been reported in numerous cancers, including breast and ovarian tumors. Alternative splicing results in several additional transcript variants, some encoding different isoforms and others that have not been fully characterized. [provided by RefSeq, Jul 2008]

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