Proxalutamide (GT0918) is a Potent Androgen Receptor (AR) Antagonist

Androgen receptors (ARs) mediate cell differentiation and development of prostate cancer. The target is a common therapeutic target in prostate cancer. Proxalutamide (GT0918) design is based on the core structure of MDV3100 but is optimized by computer-aided design. It is an innovative compound for prostate cancer and advanced breast...

Capivasertib (AZD5363) is an Orally Active pan-AKT Kinase Inhibitor

Akt/PKB (Protein kinase B), usually called Akt, is a serine/threonine protein kinase with antiapoptotic activity. In addition, Akt consists of three isoforms: PKBα/Akt1, PKBβ/Akt2 and PKBγ/Akt3. Catalytically active Akt regulates the function of numerous substrates involved in cell survival, growth, proliferation, metabolism and protein synthesis. Akt possesses a protein...

LP-261 is a Potent and Orally Active Anti-Mitotic Agent

In this article, we will introduce a potent  anti-mitotic agent, LP-261. LP-261 shows inhibition of in vitro tubulin polymerization with an EC50 of 3.2 μM. Firstly, in vitro, LP-261 exhibits potent G2/M block activity in multiple cell lines and exhibits a range of activity from 0.01 μM to 0.38 μM. Besides, the...

Venadaparib (IDX-1197) is a Potent and Selective PARP Inhibitor

PARP is an enzyme that involved in a number of cellular processes such as DNA repair, and programmed cell death. The PARP family comprises 17 members. They have all very different structures and functions in the cell. Importantly, the main role is to detect and signal single-strand DNA breaks...

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...