REDX05358 is a highly selective and potent pan RAF inhibitor with a potential therapeutic for BRAF and RAS mutant tumors. REDX05358 has improved therapeutic potential and predicted safety profile. REDX05358 demonstrates subnanomolar binding affinity for B
Protein kinase D (PKD), a serine/threonine protein kinase activated by diacylglycerol downstream of PKC signaling, has three human isoforms that modulate cell proliferation, survival, invasion, and protein transport. CRT0066101 acts as an inhibitor of these three PKD isoforms, with IC50 values of 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively. It demonstrates selectivity for PKD over a range of more than 90 protein kinases, including PKCα, PKBα, MEK, ERK, c-Raf, c-Src, and c-Abl. This specificity allows CRT0066101 to inhibit cell proliferation, induce apoptosis, and notably reduce the viability of pancreatic cancer cells both in vitro and in vivo.
AMG-628, (R)- is the R isomer of AMG-628 --- a potent, ATP-competitive inhibitor of Rafkinases. AMG-628 displays selectivity for Rafkinases and inhibits activation of tyrosine protein kinases such as VEGFR2, Lyn, Flt1 and Fms. AMG-628 has shown to inhibit growth, and induces cell cycle arrest and apoptosis in colon and melanoma cell lines with the B-RafV600E mutation.