Src inhibitor

Src inhibitor is a class of inhibitors that targets src kinase family, 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 may have prospect to be antineoplastic agents used for pancreatic cancer, breast cancer, stomach cancer et al.

chemical structure of KX2-391

Examples

• KX2-391 is an oral src inhibitor and the first clinical inhibitor with GI50 of 9–60 nM in cancer cell lines.^[1]
• 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.^[2]

chemical structure of PP1

• PP1, PP2 are both inhibitors of Lck and FynT.^[3][4]
• Quercetin
• Dasatinib

References

1. Antonarakis ES, Heath EI, Posadas EM, Yu EY, et al. (Apr 2013). "A phase 2 study of KX2-391, an oral inhibitor of Src kinase and tubulin polymerization, in men with bone-metastatic castration-resistant prostate cancer.". Cancer Chemother Pharmacol. 71 (4): 883–892. doi:10.1007/s00280-013-2079-z. PMID 23314737.
2. Nam HJ, et al. "Antitumor activity of saracatinib (AZD0530), a c-Src/Abl kinase inhibitor, alone or in combination with chemotherapeutic agents in gastric cancer.". Mol Cancer Ther. 12 (1): 16–26. doi:10.1158/1535-7163.MCT-12-0109. PMID 23144237.
3. "PP1 is a potent and selective Src inhibitor for Lck/Fyn".
4. "biological activity of PP2 in selleck chemicals". Selleck Texas.