EPI-7170 is a Potent AR N-terminal Structural Domain Antagonist
EPI-7170, a Ralaniten analogue, is a potent androgen receptor N-terminal structural domain antagonist. It blocks the transcriptional activity of full-length AR (FL-AR) and AR splice variants (AR-Vs). EPI-7170 (0-12 μM, 24 or 48 h) inhibits cell proliferation in VCaP-ENZR and C4-2B-ENZR cells. Additionally, it also enhances the effect of Enzalutamide which has...
Ulixertinib is an Orally Active and ATP-Competitive ERK1/2 Inhibitor
Effective treatment for pancreatic ductal adenocarcinoma (PDAC) is an urgent, unmet medical need. Targeting KRAS, the oncogene that is present in >95% of PDAC, is a heavily pursued strategy but remains unsuccessful in the clinic. RAF or MEK inhibitors have failed to show clinical efficacy in PDAC. A report...