non–small-cell lung cancer

Matrine (Vegard), an alkaloid isolated from the Sophora genus, acts as a kappa opioid receptor agonist.

CG347B is a selective inhibitor of HDAC6.

Oritinib (SH-1028) is an inhibitor of EGFR with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM for EGFR (wt), EGFR (L858R), EGFR (L861Q), EGFR (L858R/T790M), EGFR (d746-750), EGFR (d746-750/T790M), respectively. Oritinib can be used in studies about the treatment of non-small cell lung cancer.

Almonertinib mesylate is an irreversible inhibitor of EGFR tyrosine kinase with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate can be used in the non-small cell lung cancer studies.

Olomoucine is an ATP-competitive inhibitor of Cdk2/cyclin A, Cdc2/CyclinB, CDK2/CyclinE, CDK5/p35, and ERK1/p44 MAP kinase with IC50s of 7, 7, 7, 3, and 25 µM, respectively. It regulates the cell cycle and exhibits anti-melanin tumor activities.

Nivolumab is a monoclonal antibody and is a humanized PD-1 antibody. Nivolumab has anti-tumor activity and is used in the treatment of melanoma, non-small cell lung cancer, renal cell carcinoma, etc.

Tilatamig samrotecan (AZD9592) is an antibody-drug conjugate (ADC) delivering a topoisomerase I (TopoI) inhibitor that targets EGFR and c-MET, inducing DNA double-strand breaks and inhibiting the growth of non-small cell lung cancer cells.

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.

Divarasib (GDC-6036) is an investigational, oral, high-potency and selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib irreversibly locks KRAS G12C oncoprotein in an inactive state and inhibits tumor cell growth. It is being investigated for use in solid tumors, including non-small cell lung and colorectal cancers and other types of cancer.

5-O-Caffeoylshikimic acid is a caffeoylated derivative of shikimic acid and belongs to the class of natural polyphenolic compounds; it is widely found in plants such as Smilax glabra. 5-O-Caffeoylshikimic acid exhibits antioxidant and anti-inflammatory activity. 5-O-Caffeoylshikimic acid can be used in research related to non-small cell lung cancer (NSCLC).

Wighteone (Erythrinin B) is a small molecule compound derived from Genista ephedroides with potential antifungal and anticancer activity against EGFR L858R/T790M mutant non-small cell lung cancer.

MK-8033 hydrochloride is an effective and orally active dual inhibitor of ATP competitive c-Met/Ron, with 1 nM for c-Met and 7nM for Ron IC50. MK-8033 hydrochloride has a high affinity for activated kinase conformation, and is suitable for the study of breast cancer, bladder cancer, and non-small cell lung cancer (NSCLC).

Conteltinib (CT-707) is an enzyme inhibitor with antitumor activity targeting FAK, ALK, and Pyk2.Conteltinib exhibits significant inhibition of FAK, overcomes hypoxia-mediated sorafenib resistance in hepatocellular carcinoma through inhibition of YAP signaling, and can be used in advanced ALK-positive non-small-cell lung cancer and lymphoma.

Debio 0932 (CUDC-305) is a heat shock protein 90 (Hsp90) inhibitor that targets the n-terminal atp-binding pocket to promote apoptosis, and has the advantage of being orally available and able to cross the blood-brain barrier (BBB) for the treatment of cancers such as non-small-cell lung cancer (NSCLC) and neuroblastoma.

Antroquinonol ((+)-Antroquinonol) is a natural product and an activator of the Nrf2 signaling pathway, exhibiting anti-inflammatory, antioxidant, and anticancer activities. The compound is cell-permeable and can be used in research on non-small cell lung cancer and colon cancer. Antroquinonol has also shown potential in inhibiting inflammation and fibrosis in models of focal segmental glomerulosclerosis.

PRLX-93936 HCL is an analog of erastin and demonstrated synergistic effects against non-small cell lung cancer (NSCLC) cells with cisplatin.

KER047 (ALK2-IN-4) is an ALK2 inhibitor with potential anticancer activity and can be used in the study of non-small cell lung cancer.

USP15-IN-1 is a potent USP15 inhibitor (IC50 is 3.76 μM) with high antiproliferative activity against non-small cell lung cancer and leukemia cells. As an interacting protein of cGAS, USP15 promotes cGAS to recognize DNA and activate downstream signaling pathways.

ULK1-IN-2 is a potent ULK1 inhibitor with potential anticancer activity, inducing apoptosis while blocking autophagy.ULK1-IN-2 has high cytotoxicity against cancer cells, with an IC50 value of 1.94 μM against A549 cells.ULK1-IN-2 can be used for the study of non-small-cell lung cancer.

OTUB1/USP8-IN-1 is a potent OTUB1/USP8 inhibitor with potential anticancer activity, demonstrating IC50 values of 0.17 nM for OTUB1 and 0.28 nM for USP8. OTUB1/USP8-IN-1 can be used in the study of non-small-cell lung cancer.

Akt3 degrader 1 is a specific Akt3 degrader with anticancer and antiproliferative activity that inhibits tumor growth in mice.Akt3 degrader 1 is used in the study of non-small cell lung cancer and pancreatic cancer.

iMDK quarterhydrate is a potent PI3K inhibitor that inhibits the growth factor MDK (also known as midkine or MK). iMDK quarterhydrate synergistically inhibits non-small cell lung cancer (NSCLC) with MEK inhibitors without harming normal cells and mice.

Pemetrexed disodium (LY-231514) is a parenterally administered folate antagonist and antineoplastic agent, used in the treatment of non-small cell lung cancer and malignant mesothelioma. Pemetrexed disodium therapy has been associated with moderate rates of serum enzyme elevations during therapy, but has not been convincingly linked to instances of acute, clinically apparent liver injury.

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