non-small

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

Gefitinib (ZD1839) is an EGFR first-generation inhibitor with oral activity that inhibits the EGFR 19 Del and L858R mutations. Gefitinib has antitumor activity and is used for the treatment of EGFR-mutated non-small-cell lung cancers. Gefitinib administration RESULTS in the development of the EGFR C797S resistance mutation.

KSQ-4279 (USP1-IN-1) is an inhibitor of USP1 and PARP, exhibiting anticancer activity. It is utilized in the study of non-small cell lung cancer, osteosarcoma, ovarian, breast, glioblastoma, bladder, uterine, and pancreatic cancers.

VX-984 (M9831) is an oral, selective DNA-PK inhibitor that can cross the blood-brain barrier. VX-984 inhibited the conjugation of non-homologous terminal NHEJ and acted on DSBs to break DNA double strand. VX-984 is commonly seen in glioblastoma (GBM) and non-small cell lung cancer (NSC-LC) studies.

Nivolumab is a monoclonal antibody, a humanized IgG4 antibody to PD-1. Nivolumab has antitumor activity and is used in the treatment of melanoma, non-small cell lung cancer, renal cell carcinoma and others.

Tepotinib (EMD-1214063) is a c-MET tyrosine kinase inhibitor (IC50=3 nM) that is selective, orally active, and ATP-competitive. Tepotinib has antitumor effect and is used in the treatment of non-small cell lung cancer.

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) (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.

Amivantamab (JNJ-61186372) is a humanized antibody that recognizes epidermal growth factor receptor (EGFR) and MET proto-oncogene (MET), with anticancer and anti-tumor activities, preventing ligand binding to EGFR and MET and receptor dimerization that inhibits downstream signal transduction. Amivantamab can induce Fc-dependent endocytosis of macrophages and antibody-dependent cytotoxicity of natural killer cells, and can be used to study metastatic non-small cell lung cancer.

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.

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.

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.

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.

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.

5-A-RU (5-Amino-6-(D-ribitylamino)uracil) is an early intermediate in riboflavin biosynthesis and is found in a variety of bacteria and yeast as well as plants. 5-A-RU is also a mucosal-associated invariant T (MAIT) cell activator that forms potent MAIT-activating antigens through non-enzymatic reactions with small molecules from other metabolic pathways.

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.

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.

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.

(1S,2R)-2-PCCA is a novel and potent small molecule GPR88 receptor agonist with an EC50 value of 3 nM in the non-cellular system and 603 nM in the cellular system.

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

CUR61414 hydrochloride is a potent and cell permeable inhibitor of Hedgehog signaling pathway (IC50 =100-200 nM). CUR61414 hydrochloride is a small-molecule aminoproline class compound. CUR61414 hydrochloride selectively binds to smoothened (Smo, Ki= 44 nM). CUR61414 hydrochloride can induce cancer cells apoptosis without affecting neighboring non-tumor cells.

Pegamotecan (PEG-camptothecin) is a topoisomerase I (TOP1) inhibitor with anticancer activity, and it is used in the treatment of esophageal, non-small cell lung and pancreatic cancers.

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).

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.