Rociletinib (CO-1686) is an Orally Active EGFR-Mutant Inhibitor
NSCLC accounts for almost 85% of all lung cancers. Additionally, lung cancer continues to be the most common cause of cancer-related deaths worldwide. Activating mutations in the epidermal growth factor receptor (EGFR) are key drivers of NSCLC malignancy. Patients with the most common EGFR mutations (L858R mutation in exon...
Motesanib is a potent ATP-Competitive Inhibitor of VEGFR1/2/3
There are numerous growth factors involved in tumor angiogenesis, but foremost among them is the family of vascular endothelial growth factors (VEGFs). The VEGF family includes VEGFA, VEGFB, VEGFC, VEGFD, and placenta growth factor (PGF). These ligands bind with different affinities to three endothelial receptor tyrosine kinases (RTKs), such...
Vorasidenib (AG-881) is an Orally Available, Brain Penetrant and dual mIDH1/2 Inhibitor
Isocitrate dehydrogenases 1 and 2 (IDH1/2) are homodimeric enzymes. They catalyze the conversion of isocitrate to α-ketoglutarate (α-KG) in the tricarboxylic acid cycle. However, mutant IDH1/2 (mIDH1/2) reduces α-KG to the oncometabolite 2-hydroxyglutarate (2-HG). Inhibition of the mutant IDH (mIDH) protein represents a targeted approach to cancer treatment for...
Golvatinib (E-7050) is a potent Dual Inhibitor of both c-Met and VEGFR2 Kinases
c-Met is the cellular receptor for the hepatocyte growth factor (HGF). Activation of the HGF⁄c-Met pathway always leads to tumor progression, invasion, and metastasis. Vascular endothelial growth factor (VEGF) is an important molecule in tumor progression. Additionally, VEGF is associated with tumor angiogenesis. Due to their important role in...
NCGC00378430 is a Potent SIX1/EYA2 Interaction Inhibitor
The Sine oculis homeobox homolog 1 (SIX1)/eyes absent (EYA) transcription complex plays a key role in the development of multiple organs. Specifically, members of the SIX gene family encode proteins characterized by different DNA binding homologous domains and upstream six domains. This may involve determining DNA binding specificity and...
CCI-007 Possesses Anti-Cancer Activity against Infant MLL-Rearranged Leukemia
Leukemia, characterized by rearrangement of the mixed lineage leukemia (MLL) gene, is a highly aggressive cancer. And the infant leukemia is particularly common. However, the cure rate of infant leukemia has been stagnant in recent years. The occurrence of MLL gene rearrangement is a prognostic factor for high-risk diseases....
ARV-110 is an Orally Active, Specific Androgen Receptor (AR) PROTAC Degrader
Proteolysis targeting chimeras also names PROTAC protein degraders. PROTACs are emerging as an excellent class of small molecule therapies for cancer and other diseases. As we all know, conventional inhibitors or antagonists usually block the enzymatic or signaling activity of target proteins. PROTACs harness a system present within every...