Category: Non-Small Cell Lung Cancer

Rucaparib is a PARP Inhibitor

PARP is a family of proteins involved in many cellular processes, such as DNA repair, genomic stability, and programmed cell death. At least 18 members of the PARP family are encoded by different genes and have homology in conserved catalytic domains. Specifically, PARPs play an important role in various...

Repotrectinib is a potent ROS1 and TRK Inhibitor

Repotrectinib is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. The IC50 values are 0.83/0.05/0.1 nM for TRKA/B/C, respectively. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM). Repotrectinib inhibits mutant ALKs. It inhibits ALK G1202R with an IC50 of 1.26 nM. Besides, it inhibits ALK L1196M with an IC50 of 1.08 nM)....

Almonertinib is an Orally Active and Irreversible EGFR Inhibitor

Lung cancer is one of the most common malignant tumors in the world. Its lethality ranks the first among many malignant tumors. In addition, the overexpression of the human ATP-binding cassette (ABC) drug transporter ABCB1 (P-gp) or ABCG2 (BCRP) in cancer cells often contributes significantly to the development of...

Brusatol (NSC 172924) is a Nrf2 Inhibitor

Keap1-Nrf2 is the major regulator of cytoprotective responses to electrophilic chemicals or reactive oxygen species (ROS).  Upregulation of Nrf2 inducing by inactivation of Keap1 is often observed in cancer cells. Aberrant activation of Nrf2 in cancer cells accelerates proliferation and metabolism. Meanwhile, Nrf2 is a transcription factor that regulates cellular...

Ganetespib (STA-9090) is a HSP90 Inhibitor

Hsp90 is a molecular chaperone that regulates the posttranslational folding, stability, and function of its protein substrates (client proteins), many of which play critical roles in cell growth, differentiation, and survival. The Hsp90 machinery serves as a biochemical buffer for a number of oncogenic signaling proteins causally implicated in...

Elesclomol (STA-4783) is an Oxidative Stress Inducer and Induces Apoptosis

Modulating reactive oxygen species (ROS) levels has been proposed as a therapeutic strategy for cancer. In normal cells, ROS are produced at low concentrations and cancer cells produce elevated levels of ROS due to increased metabolic activity, resulting in a state of chronic oxidative stress. Recent studies showed the...