nsclc cells

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

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.

Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.

RMC5127 is an oral and mutation-selective inhibitor of RASG12V (ON) that inhibits the GTP-bound (ON) form of RAS G12V through the formation of a high-affinity triplex with central nervous system (CNS) permeability and brain permeability. RMC5127 inhibits RAS pathway activity in vitro in KRAS G12V mutant human cancer cells and cellular proliferation, and antitumor activity in preclinical intracranial xenograft models and subcutaneous CDX and PDX models of KRAS G12V mutant NSCLC, PDAC and CRC.

Peruvoside (Encordin) is a natural cardiac glycoside that inhibits Na+/K+-ATPase to increase myocardial contractility; causes cell cycle arrest in leukemia stem cells at the G₂/M phase, and; inhibits NSCLC cell growth as a Src inhibitor; and induces apoptosis in cancer cells through MAPK Wnt / β-catenin and PI3K / AKT / mTOR .

ES-072, a selective inhibitor targeting the EGFR mutant (EGFR-T790M), is administered orally. By hindering EGFR-T790M activity, it activates GSK3α, which subsequently leads to the phosphorylation of PD-L1 at Ser279 and Ser283. This phosphorylation facilitates the recruitment of the E3 ubiquitin ligase ARIH1, resulting in the ubiquitination and proteasomal degradation of PD-L1. Such a process not only curtails the growth of cancer cells but also amplifies the anti-tumor immune response by diminishing PD-L1 levels. ES-072 has shown efficacy in impeding the proliferation of non-small cell lung cancer (NSCLC) cells.

NHTD, a KRAS-PDEδ inhibitor, exerts its function by targeting the isoprenyl binding pocket of PDEδ, which alters the cellular localization of KRAS. This modification restricts the proliferation of cancer cells with KRAS mutations and induces cell apoptosis (Apoptosis). NHTD is utilized in the study of KRAS-driven non-small cell lung cancer (NSCLC).

And1 degrader 1 (Compound A15) is a degrader of acidic nucleoplasmic DNA-binding protein 1 (And1) that notably induces degradation of And1 in NSCLC cells. When combined with Olaparib (1 μM), And1 degrader 1 at a concentration of 5 μM effectively inhibits proliferation in A549 and H460 cells. This compound is applicable in cancer research studies.

Top HDAC-IN-3 (Compound 31) is a dual inhibitor of Topoisomerase and HDAC with oral activity. It induces DNA damage by elevating reactive oxygen species (ROS) levels, consequently inhibiting the clonal formation and migration of cancer cells, and triggering apoptosis (Apoptosis) and cell cycle arrest. Top HDAC-IN-3 demonstrates a significant antitumor effect in NSCLC models, exhibiting a tumor growth inhibition (TGI = 77.5%, 100 mg kg) superior to that of the HDAC inhibitor SAHA and the combination of SAHA with the topoisomerase inhibitor Irinotecan.

NA-17 is a naphthalimide compound with antitumor activity and exhibits lower toxicity to normal cells such as HL-7702 and WI-38. It demonstrates p53-dependent inhibition selectivity in various NSCLC cells, inducing the accumulation of active p53 in the mitochondria and nuclei of these cells. NA-17 causes cell cycle arrest in the G1 phase and promotes apoptosis and cell death.

EGFR-IN-139 (compound PD 18) is an EGFR inhibitor with IC50 values of 12.88 nM (wild type), 10.84 nM (L858R T790M), and 42.68 nM (L858R T790M C797S). It demonstrates significant anticancer activity against the A549 and H1975 cancer cell lines, which express high levels of EGFR. EGFR-IN-139 exhibits strong selectivity for cancer cells and can be utilized in research on non-small cell lung cancer (NSCLC).

EGFRT790M L858R-IN-9 (Compound 8) is an inhibitor targeting the EGFR-L858R T790M mutations. It effectively inhibits the phosphorylation of the EGFR-L858R T790M mutant kinase, demonstrating an IC50 value of 0.0064 µM. Additionally, EGFRT790M L858R-IN-9 can suppress the proliferation of non-small cell lung cancer (NSCLC) cells, making it useful for cancer research.

PROTACROR1degrader-1 (Compound 11d) serves as a PROTAC degrader targeting the pseudokinase ROR1, with the capability of degrading ROR1 in NSCLC cells at a DC50 of 40-80 nM. It induces PARP cleavage and apoptosis in NCI-H23 cells. [Pink: ligand for target protein ROR1 ligand-1; Black: linker; Blue: ligand for VHL E3 ligase (S,R,S)-AHPC]

CDK9-IN-36 (Compound T7) is a potent, selective, and metabolically stable CDK9 inhibitor with an IC50 value of 1.2 nM. It effectively suppresses the proliferation of Osimertinib-resistant NSCLC cells by downregulating Mcl-1, reducing colony formation, and inducing apoptosis. Additionally, CDK9-IN-36 exhibits antitumor activity in xenograft models.

RET-IN-29 (Compound 8W) is a selective RET kinase inhibitor. It demonstrates inhibitory effects on BaF3 cells with the CCDC6-RETV804M mutation, with an IC50 of 0.715 μM. RET-IN-29 shows potential for research in non-small cell lung cancer (NSCLC).

anti-NSCLC agent-1 (compound 8dc) is an inhibitor of tyrosine kinase inhibitors (TKI), and demonstrates IC50 values of 0.05 μM in A549 cells and 0.09 μM in NCI-H441 cells. It exhibits anti-NSCLC activity by inhibiting colony formation, as well as cell migration and invasion.

TIP48/49-IN-1 (Compound B) is an orally active, specific RUVBL1/2 ATPase inhibitor, with an IC50 of 59 nM for purified RUVBL1/2. It disrupts the DNA replication process, causing S phase arrest, induces apoptosis, inhibits tumor growth, and enhances the radiosensitivity of non-small cell lung cancer cells (NSCLC).

EGFR-IN-150 is an EGFR inhibitor that effectively inhibits the phosphorylation of mutant epidermal growth factor receptor (EGFR) and its downstream AKT signaling pathway, exerting antitumor effects and inducing HMOX1 expression to trigger ferroptosis. This compound exhibits an IC50 of 0.386 μM against the non-small cell lung cancer (NSCLC) cell line H1975 and significantly suppresses the colony formation and migration abilities of H1975 and A549 cells, while also inducing apoptosis. Additionally, EGFR-IN-150 prominently reduces tumor growth in H1975 tumor-bearing mouse CDX models. It holds promise for research related to non-small cell lung cancer.

HSND80 (Compound 1) is an orally active MNK/p70S6K inhibitor, exhibiting a Kd value of 44 nM for MNK1 and 4 nM for MNK2. The residence time of HSND80 on MNK1 and MNK2 is 45 minutes and 58 minutes, respectively. HSND80 effectively inhibits non-small cell lung cancer (NSCLC) both in vitro and in vivo, and suppresses the growth of triple-negative breast cancer (TNBC) cells in vitro.

Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27) is an active molecular conjugate used in antibody-drug conjugates (ADCs), consisting of the ADC linker Mal-N(Me)-C6-N(Me) and the potent cytotoxin PNU-159682. This compound selectively delivers its payload to cells expressing CD46 and releases PNU-159682 through cathepsin B cleavage of the linker, inducing DNA damage and apoptosis. Mal-N(Me)-C6-N(Me)-PNU-159682 has demonstrated sustained tumor regression in patient-derived xenograft (PDX) models of non-small cell lung cancer (NSCLC) and colorectal cancer (CRC).

ALK-IN-31 (Compound Ld-10) is an orally active ALK inhibitor with an IC50 of 1135 nM. It demonstrates excellent antiproliferative activity against lung cancer cells H2228, with an IC50 value of 1.35 μM. ALK-IN-31 induces apoptosis and arrests cell proliferation at the G0/G1 phase by affecting mitochondrial function. It exhibits antitumor effects by downregulating the expression of p-AKT and p-mTOR in the PI3K-AKT-mTOR signaling pathway downstream of ALK. This compound is applicable for research into non-small cell lung cancer (NSCLC).

FAK-IN-27 (compound 8A) is a potent and selective inhibitor of FAK, with an IC50 of 4.968 nM. It effectively inhibits the proliferation of H1299 cells, with an IC50 of 0.28 μM, and is applicable for research in non-small cell lung cancer (NSCLC).

TrxR-IN-8 (Compound 6f) is a selective inhibitor of TrxR with an IC50 of 10.2 μM. It induces apoptosis through oxidative stress by stimulating the production of reactive oxygen species, reducing intracellular thiols, and lowering the glutathione/glutathione disulfide ratio. TrxR-IN-8 exhibits significant cytotoxicity against non-small cell lung cancer (NSCLC) cells.

Dornidazole (PR-000350, PR-350, RP-343, PR-69) is an effective radiosensitizer for hypoxic cells with the potential for the treatment of non-small cell lung cancer (NSCLC) and pancreatic cancer.