GNE-9815 is a highly selective pan-RAF inhibitor, can be used to research KRAS mutant cancers
Rapidly accelerated fibrous sarcoma (RAF) kinases are a family of three serine/threonine-specific protein kinases associated with retroviral oncogenes. They play key roles in several cellular processes, including cell cycle progression, cell proliferation, cell metabolism, cell migration, cell differentiation, and apoptosis. Activation of RAF kinases requires interaction with RAS-GTPases. RAF...
Ravoxertinib is an Orally Active and Highly Selective ERK1/2 Inhibitor
The RAS/RAF/MEK/ERK (MAPK) signal transduction pathway has attracted significant interest as a therapeutic target for cancer. ERK1/2 phosphorylates more than 50 downstream substrates responsible for cell growth, proliferation, survival, angiogenesis, and differentiation. Small molecule inhibitors of BRAF and MEK have shown promising activities in a variety of solid tumors...
LY3214996 an Orally Active ERK1/2 Inhibitor with Potential Antineoplastic Activity
The Ras/Raf/MEK/ERK signaling cascade integrates extracellular clues from cell surface receptors to gene expression and regulation of multiple cellular proteins. Extracellular-signal-regulated kinases (ERKs) serve as key central nodes within this pathway. Simultaneous targeting of multiple effectors such as RAF, MEK, and ERK offers the potential for enhanced efficacy while...
SCH772984 is an ATP Competitive and Non-Competitive ERK1 and ERK2 Inhibitor
Specific inhibitors of RAF and MEK kinases to target BRAF– and RAS-mutant tumors are developing. Interestingly, BRAF/MEK inhibitor combination treatment blocks phosphorylated extracellular signal-regulated kinase (phospho-ERK) reactivation in melanoma cells, a phenomenon that may possibly reduce the emergence of clinical resistance. ERK represents an attractive downstream target to exploit. SCH772984...
AZ304, a Dual BRAF Inhibitor Against Cancer
Cancer is the most serious disease in the world. Gene mutation always exhibits in many of human cancers, especially oncogenic BRAF mutations. Non-small cell lung cancer, ovarian cancer, leukaemia, gliomas and other malignancies have had BRAF mutations already. Although several BRAF inhibitors are launched to market, we need to...