Src inhibitor

Src inhibitor is a class of inhibitors that targets src kinase family of tyrosine kinases, which is transcribed by proto-oncogenes src genes (abbreviating for sarcome genes) that potentially induced cell of malignant transformation. Because of the crucial position of src gene/kinase in cells, src inhibitors are potential antineoplastic agents for pancreatic cancer, breast cancer, stomach cancer etc.^[1]

chemical structure of KX2-391

Examples[]

• is an oral src inhibitor and the first clinical inhibitor with GI50 of 9–60 nM in cancer cell lines.^[2]
• Bosutinib has been developed for the treatment of chronic myelogenous leukemia by Pfizer.
• Saracatinib, the first Src inhibitor to show inhibition of the Src pathway in human tumor tissue, has anti-tumor activity alone or in combination with chemotherapeutic agents.^[3]

chemical structure of PP1

• PP1, PP2 (kinase inhibitor) are both inhibitors of Lck and FynT.^[4][5]
• Dasatinib^[1][6]

References[]