Category: Non-Small Cell Lung Cancer

Seliciclib (Roscovitine) is an Orally Active and Selective CDKs Inhibitor

Cyclin-dependent kinases (CDKs) are serine/threonine kinases whose activity depends on a regulatory subunit-a cyclin. Based on the sequence of the kinase domain, CDKs belong to the CMGC group of kinases, along with MAPKs, Gsk3β, DYRK family and CDK-like kinases. There are around 20 Cyclin-dependent kinases (CDK1-20) known till date....

Rigosertib is a Multi-Kinase Inhibitor and a Selective Anti-Cancer Agent

Polo-like Kinases (PLKs) are a group of highly conserved serine/threonine protein kinases. PLKs play a key role in processes such as cell division and checkpoint regulation of mitosis. Mammalian cells contain at least four members of Plk gene family, termed Plk1, Plk2 (also known as Snk), Plk3 (also known...

Avitinib is an Irreversible, Mutant-Selective EGFR Inhibitor

The epidermal growth factor receptor (EGFR) belongs to the ErbB family (also known as the EGFR family) of receptor tyrosine kinases (RTK). EGFR family comprises four distinct receptors: the EGFR (ErbB1, HER1), ErbB-2 (HER2, neu in rodents), ErbB-3 (HER3) and ErbB-4 (HER4). It is worth mentioning that EGFR family...

Indoximod, An Immunometabolic Adjuvant, is an IDO Pathway Inhibitor

Indoleamine 2,3-dioxygenase (IDO) is an enzyme of interest in immuno-oncology. It has immunosuppressive effects that result from its role in tryptophan catabolism. IDO1 catalyzes the initial rate-limiting step in the degradation of the essential amino acid tryptophan along the kynurenine pathway. IDO inhibits a tryptophan sufficiency signal that stimulates...

GS-493 is a Selective Protein Tyrosine Phosphatase SHP2 (PTPN11) Inhibitor

The protein tyrosine phosphatase SHP2 (also called SH-PTP2, Syp, PTP1D, and PT-P2C) is a ubiquitously expressed 68 kDa non-receptor PTP. In the inactive state, the SH2 domains of SHP2 auto-inhibit the catalytic PTP domain by binding intramolecularly to the defined acidic residues. Upon activation, several receptor tyrosine kinases, including MET,...

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)....