BMS-754807 химические свойства, назначение, производство
Описание
BMS 754807 is a reversible, orally bioavailable dual inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (InsR) tyrosine kinases (IC50s = 1.8 and 1.7 nM, respectively). It has minimal effect against an array of other tyrosine and serine/threonine kinases. BMS 754807 inhibits cell proliferation or induces apoptosis in a variety of cancer cells in vitro. It inhibits the growth of tumor xenografts in mice and this effect is often enhanced by combination therapy with other chemotherapeutics. Predictive biomarkers, including elevated IGF-1R expression, for effectiveness of BMS 754807 have been delineated.
Использование
BMS-754807 has been used in the embryo drug treatment.
Общее описание
BMS-754807 is a pyrrolotriazine, which is a potent dual inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (InsR) tyrosine kinase. It has been reported that BMS-754807 also acts as a reversible ATP-competitive antagonist of IGF-1R by restricting the catalytic domain of the IGF-1R.
BMS-754807 препаратная продукция и сырье
сырьё
препарат