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.

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.

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.

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

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

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

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.

Antitumor agent-135 (Compound 13) is an effective anticancer drug that induces apoptosis. It exhibits IC50 values of 3.79, 10.55, 1.14, and 4.14 μM against NSCLC cell lines (A549, H460, PC-9, and PC-9/GR), respectively.

SOS1/EGFR-IN-1 (compound SE-9) is a dual-target inhibitor for prostate cancer, effectively suppressing downstream effector molecules through the inhibition of SOS1 and EGFR. It induces apoptosis and G1 phase cell cycle arrest, reducing angiogenesis and migration. In prostate cancer cells PC-3, it demonstrates significant antitumor activity with an IC50 of 0.45±0.03 μM.

Panduratin A is a natural chalcone derivative with inhibitory activity against MMP-9 in human oral epidermoid carcinoma KB cells; inhibitory activity against the NS3 protease of DENV-2 (Ki=25 μM); significant cytotoxicity against human androgen-independent prostate cancer cells PC-3 and DU-145; and also able to activate the LKB1-AMPK- PPARα /δ signaling pathway and enhance the oxidative capacity of myocyte mitochondria.

Ensartinib (X-396) is a potent and orally active dual ALK MET inhibitor for the treatment of ALK-positive non-small cell lung cancer (NSCLC).

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).

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].

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.

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.

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.