pc-9

Osimertinib (AZD-9291) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.

DPC-961, a reverse transcriptase inhibitor, is used potentially for the treatment of HIV infection.

DPC-963 is a RNA-directed DNA polymerase inhibitor.

Acetylcysteine (NAC) is an N-acetyl derivative of cysteine, a ROS inhibitor and mucolytic agent. Acetylcysteine induces apoptosis, can be used to reduce mucus thickness, and has anti-influenza viral activity.

Osimertinib mesylate (AZD-9291 mesylate) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib mesylate has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.

Erlotinib (NSC-718781) is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer.

Ensartinib (X-396) is a potent dual ALK MET inhibitor with IC50 values of <0.4 nM for ALK and 0.74 nM for MET.

Zipalertinib (TAS6417, CLN-081) is a novel, highly potent, orally active covalent EGFR tyrosine kinase inhibitor that uniquely binds to the ATP binding site of the EGFR hinge region with an IC50 value of 1.1-8.0 nM.

PC-M5' is a natural product that can be used as a reference standard. The CAS number of PC-M5' is 133613-75-9.

EGFR-IN-117 (Compound 8h) exhibits inhibitory activity against EGFR mutations, specifically targeting the tumor environment and inducing apoptosis in cancer cells. This compound effectively inhibits the proliferation of H1975, PC-9, and mutant EGFR cells including BaF3-EGFRL858R T790M C797S and BaF3–C797S Del19 T790M, with IC50 values of 13 nM, 19 nM, 1.2 nM, and 1.3 nM respectively. Additionally, EGFR-IN-117 demonstrates anti-tumor activity in mouse models.

PROTAC EGFR degrader 8 (T-184) is a PROTAC that selectively degrades the epidermal growth factor receptor (EGFR) with a DC50 of 15.56 nM in HCC827 cells, and inhibits the growth of cell lines H1975, PC-9, and HCC827 with IC50 values of 7.72 nM, 121.9 nM, and 14.21 nM, respectively. This compound is used primarily for cancer research, particularly in the context of non-small cell lung cancer (NSCLC) [1].

D609 (Tricyclodecan-9-yl-Xanthogenate) has a wide range of biological activities including antioxidant, antiapoptotic, anticholinergic, antitumor, anti-inflammatory, antiviral, antiproliferative, and neuroprotective activities.D609 acts by inducing competitive inhibition of PC-specific phospholipase C (PC-PLC) and sphingomyelin synthase (SMS). D609 acts by causing competitive inhibition of PC-specific phospholipase C (PC-PLC) and sphingomyelin synthase (SMS).

AKV-9 is an inhibitor of mutant Cu Zn superoxide dismutase (SOD1), effectively preventing SOD1-induced protein aggregation and providing protection against SOD1-induced cytotoxicity in PC-12 cells, with an EC50 of 0.3 μM. Additionally, AKV-9 has been shown to improve amyotrophic lateral sclerosis (ALS) in mouse models and extend their lifespan.

B-Raf IN 9 (compound 8b) is an effective B-Raf inhibitor (IC50=24.79 nM) that blocks the cell cycle at the G2 M phase, induces apoptosis, and exhibits potent anti-tumor activity on human prostate cancer PC-3 cells (IC50=7.83 μM).

PON-PC, an oxidized phospholipid with a 9-carbon fatty acyl chain ending in an aldehyde at the sn-2 position, arises from the oxidation of palmitoyl oleoyl phosphatidylcholine (POPC) or through interaction with ozone in pulmonary surfactant. It is found in oxidized LDL. At a 40 µM concentration, PON-PC diminishes the production of TNF-α, nitric oxide (NO), and NADP+ in primary mouse alveolar macrophages and lowers the bactericidal capability of RAW 264.7 cells. Additionally, levels of PON-PC increase in the bronchoalveolar lavage fluid (BALF) of mice exposed to cigarette smoke or in older mice.

YS-67 is an orally available, selective and potent EGFR inhibitor with antitumor activity, inhibits p-EGFR and p-AKT, and inhibits the proliferation of A549, PC-9, and A431 cells.YS-67 blocks cell cycle progression and induces apoptosis in the G0 G1 phase, and can be used in the study of non-small-cell lung cancer.