Description
PP-242 is an inhibitor of mTORC1/2 that displays anticancer chemotherapeutic and anti-metastatic activities. In various cellular models of acute leukemia, PP-242 inhibits cell proliferation. In animal models of pheochromocytoma, PP-242 induces apoptosis, upregulates expression of Bax, downregulates expression of Bcl-2, and decreases tumor volume. In gastric cancer cells, this compound also inhibits cell proliferation, migration, and invasion and suppresses tube formation and vascular invasion.
References
Shi F, Yang X, Gong Y, et al. The antileukemia roles of PP242 alone or in combination with daunorubicin in acute leukemia. Anticancer Drugs. 2015 Apr;26(4):410-21. PMID: 25535978.
Zhang X, Wang X, Qin L, et al. The dual mTORC1 and mTORC2 inhibitor PP242 shows strong antitumor activity in a pheochromocytoma PC12 cell tumor model. Urology. 2015 Jan;85(1):273.e1-7. PMID: 25440763.
Xing X, Zhang L, Wen X, et al. PP242 suppresses cell proliferation, metastasis, and angiogenesis of gastric cancer through inhibition of the PI3K/AKT/mTOR pathway. Anticancer Drugs. 2014 Nov;25(10):1129-40. PMID: 25035961.
