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NSCLC cell lines

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27

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Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-109061
    Lazertinib
    3 Publications Verification

    YH25448; GNS-1480

    		 Apoptosis Akt TRP Channel EGFR ERK Infection Neurological Disease Metabolic Disease Cancer
    Lazertinib (YH25448; GNS-1480) is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
    Lazertinib
  • HY-157229
    STX-721
    1 Publications Verification

    		 EGFR ERK Cancer
    STX-721 is an orally active, irreversible, covalent EGFR exon 20 insertion (ex20ins) inhibitor that selectively targets ex20ins-mutant dynamic protein states. STX-721 potently inhibits the kinase activity of EGFR ex20ins mutants (NPG, ASV, SVD). STX-721 inhibits phosphorylation of EGFR (pEGFR Y1068) and downstream ERK (pERK Thr202/Tyr204), and suppresses proliferation of ex20ins-mutant Ba/F3 cells and human NSCLC cell lines (NCI-H2073 ASV KI, CUTO-14 ASV). STX-721 induces tumor regression in EGFR ex20ins-mutant PDX/CDX models. STX-721 can be used for the study of non-small cell lung cancer (NSCLC) harboring EGFR or HER2 ex20ins mutations .
    STX-721
  • HY-153604
    MC4171
    2 Publications Verification

    		 Histone Acetyltransferase Cancer
    MC4171 (compound 34) is a selective KAT8 inhibitor (IC50=8.1 µM). MC4171 has been shown to exhibit moderate micromolar antiproliferative activity in different cancer cell lines, including NSCLC and AML, with potential for studying cancer .
    MC4171
  • HY-19637
    SW044248

    		Topoisomerase Cancer
    SW044248 is a non-canonical topoisomerase I inhibitor, and selectively toxic for certain non-small cell lung cancer (NSCLC) cell lines.
    SW044248
  • HY-143466
    ULK1-IN-2

    		FAK ULK AMPK Apoptosis Autophagy Cancer
    ULK1-IN-2 (compound 3s) is a potent ULK1 inhibitor. ULK1-IN-2 shows highest cytotoxic effect against cancer cell lines, with IC50 of 1.94 μM in A549. ULK1-IN-2 can induce apoptosis and simultaneously block autophagy, and can be used to study NSCLC (Non-small cell lung cancer) .
    ULK1-IN-2
  • HY-139047
    SW157765

    		GLUT Cancer
    SW157765 is a selective non-canonical glucose transporter GLUT8 (SLC2A8) inhibitor. KRAS/KEAP1 double mutant NSCLC cells are selectively sensitive to the SW157765, due to the convergent consequences of dual KRAS and NRF2 modulation of metabolic and xenobiotic gene regulatory programs .
    SW157765
  • HY-178472
    AurAP14

    		PROTACs Aurora Kinase Cancer
    AurAP14 is an Aurora A PROTAC degrader (DC50 = 120 nM). AurAP14 shows significant inhibitory activity against various tumor cell lines, with IC50s of 0.294 μM in A549 cells and 0.534 μM in MCF-7 cells. AurAP14 induces apoptosis and arrests A549 cells in the S and G2/M phases. AurAP14 demonstrates anti-tumor efficacy in nude mouse xenograft models of A549 and A549/PTR. AurAP14can be used in the research on the treatment of Aurora A-overexpressing NSCLC. (Pink: Aurora A ligand (HY-10971), Blue: E3 ligase Ligand (HY-W437598), Black: Linker) .
    AurAP14
  • HY-101522
    CHMFL-EGFR-202

    		EGFR BMX Kinase Btk MEK Cancer
    CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ～10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines .
    CHMFL-EGFR-202
  • HY-147802
    EGFR-IN-59

    		EGFR Apoptosis Cancer
    EGFR-IN-59 (Compound 8c) is a EGFR inhibitor (IC50=190 nM) and apoptosis inducer. EGFR-IN-59 exhibits cytotoxicity against non-small lung cancer cell lines (A549) and normal lung fibroblasts (WI38) with IC50s of 8.62 and 52.6 µM, respectively. EGFR-IN-59 can be used for the research of various cancers such as non-small cell lung cancer (NSCLC), head and neck cancer, breast cancer and colorectal cancer .
    EGFR-IN-59
  • HY-148572
    NAMPT/IDO1-IN-1

    		Indoleamine 2,3-Dioxygenase (IDO) NAMPT Cancer
    NAMPT/IDO1-IN-1 is an orally active dual inhibitor of NAMPT and IDO1 with IC50s of 57.7 nM and 233 nM, respectively. NAMPT/IDO1-IN-1 blocks NAD+ biosynthesis, inhibits proliferation and migration of Paclitaxel (HY-B0015)- and FK866 (HY-50876)-resistant NSCLC cell lines (A549/R cells). NAMPT/IDO1-IN-1 has shown antitumor effects in mice and enhanced A549/R cell sensitivity to paclitaxel .
    NAMPT/IDO1-IN-1
  • HY-174088
    CDK4/6/BRD4-IN-2

    		CDK Discoidin Domain Receptor Apoptosis Reactive Oxygen Species (ROS) DNA/RNA Synthesis Cancer
    CDK4/6/BRD4-IN-2 (Compound PJ2) is a dual inhibitor of CDK4/6 and BRD4 with IC50 values for CDK4, CDK6, BRD4 (BD1), and BRD4 (BD2) of 168.75, 292.45, 23.17, and 3.12 nM respectively. CDK4/6/BRD4-IN-2 has a strong inhibitory effect on non-small cell lung cancer (NSCLC) cell lines. CDK4/6/BRD4-IN-2 induces cell cycle arrest, senescence and apoptosis through ROS-mediated DNA damage. CDK4/6/BRD4-IN-2 can also effectively inhibit the migration and invasion of NCI-H358 cells. CDK4/6-IN-2 can be used for the study of KRAS-mutated NSCLC .
    CDK4/6/BRD4-IN-2
  • HY-105369
    KF-20444

    		Anaplastic lymphoma kinase (ALK) Apoptosis Cancer
    KF-20444 is an orally active ALK inhibitor with blood-brain barrier penetration. KF-20444 exhibits strong inhibitory activity against ALK fusion proteins (EML4-ALK) and ALK resistance mutations (including L1196M, G1202R, and F1174L). KF-20444 effectively suppresses the phosphorylation of ALK in ALK-driven cancer cell lines, thereby inhibiting cancer cell proliferation and inducing apoptosis. KF-20444 demonstrates anti-tumor efficacy in mouse models bearing ALK-positive non-small cell lung cancer (NSCLC) or neuroblastoma. KF-20444 can be used for the study of ALK-driven malignancies .
    KF-20444
  • HY-178057
    EGFR-IN-176

    		EGFR Akt Anaplastic lymphoma kinase (ALK) Apoptosis Cancer
    EGFR-IN-176 is an orally active and ATP-competitive EGFR mutant inhibitor (particularly C797S-mediated EGFR triple mutant). EGFR-IN-176 effectively inhibits subsequent AKT signaling and induces apoptosis in Ba/F3 and PC-9 cells expressing EGFR 19del/T790M/C797S and EGFR L858R/T790M/C797S. EGFR-IN-176 selectively inhibits EGFR signaling in cell lines harboring EGFR triple mutation and shows no inhibitory effect against A431 cells that express wild-type EGFR. EGFR-IN-176 can effectively inhibit the enzymatic activity of ALK (IC50 < 0.5 nM). EGFR-IN-176 can be used for the study of non-small cell lung cancer (NSCLC) .
    EGFR-IN-176
  • HY-162098
    PROTAC tubulin-Degrader-1

    		PROTACs Microtubule/Tubulin Apoptosis Cancer
    PROTAC tubulin-Degrader-1 is a α/β/β3-tubulin PROTAC degrader. PROTAC tubulin-Degrader-1 exhibits potent anti-proliferative activity against multiple human tumor cell lines. PROTAC tubulin-Degrader-1 induces G2/M phase arrest and apoptosis and inhibits colony formation in A549 and A549/Taxol cells. PROTAC tubulin-Degrader-1demonstrates potent anti-tumor efficacy in A549 and A549/Taxol (Taxol-resistant) xenograft model. PROTAC tubulin-Degrader-1 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: Tubulin ligand (HY-N2146), Blue: CRBN Ligand (HY-10984), Black: Linker (HY-N6056)) .
    PROTAC tubulin-Degrader-1
  • HY-N13164
    Polygalacin D3

    		PI3K Akt Apoptosis Cancer
    Polygalacin D3 is a triterpenoid saponin compound that can be extracted from the roots of the balloon flower. Polygalacin D3 can inhibit the proliferation of non-small cell lung cancer (NSCLC) cell lines by blocking the PI3K/Akt pathway, and it induces cell cycle arrest and cell apoptosis .
    Polygalacin D3
  • HY-157564
    Antitumor agent-135

    		Apoptosis Cancer
    Antitumor agent-135 (Compound 13) is a potent antitumor agent. Antitumor agent-135 induces cell apoptosis, with IC50s of 3.79 , 10.55, 1.14, and 4.14 μM for NSCLC cell lines (A549, H460, PC-9, and PC-9/GR) .
    Antitumor agent-135
  • HY-119694
    Rotenolone

    		Fungal Cancer
    Rotenolone is an antiproliferative agent. Rotenolone shows antiproliferative activity against the ovarian cancer A2780, breast cancer BT-549, prostate cancer DU 145, NSCLC NCI-H460, and colon cancer HCC-2998 cell lines, with IC50s of 0.95, 1.6, 2.7, 2.0, and 2.9 μM, respectively .
    Rotenolone
  • HY-172449
    GLI1-IN-3

    		Hedgehog Cancer
    GLI1-IN-3 (Compound 11a), a triterpenoid analogue, can inhibit Hedgehog signaling in GLI1 overexpression cancer cells. GLI1-IN-3 inhibits the proliferation in NSCLC and prostate cancer cell lines exhibiting hyper-activated Hh signaling. GLI1-IN-3 can also decrease the expression of endogenous GLI1 protein and its target genes associated with tumor progression and proliferation in A549 and DU-145 cancer cells .
    GLI1-IN-3
  • HY-172881
    PKM2-IN-10

    		Pyruvate Kinase Cancer
    PKM2-IN-10 (Compound 16) is a PKM2 inhibitor. PKM2-IN-10 inhibits the proliferation of A549 and HCC1833 cell lines with IC50 of 3.36 μM and 9.20 μM, respectively. PKM2-IN-10 exhibits antitumor activity in human non-small cell lung cancer (NSCLC) and mouse lung adenocarcinoma models. PKM2-IN-10 can be used in lung cancer research .
    PKM2-IN-10
  • HY-12965B
    (Z)-S49076 hydrochloride

    		TAM Receptor Cancer
    (Z)-S49076 hydrochloride is an orally active inhibitor of MET and AXL that blocks the downstream signaling of these receptors both in vitro and in vivo, inhibiting the proliferation and migration of tumor cells and suppressing tumor growth in xenograft models. (Z)-S49076 hydrochloride is capable of overcoming the resistance to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) due to MET amplification in Erlotinib (HY-50896)-resistant cell lines both in vitro and in vivo. (Z)-S49076 hydrochloride can be used for research in non-small cell lung cancer (NSCLC) .
    (Z)-S49076 hydrochloride
  • HY-170438
    EGFR-IN-139

    		EGFR Cancer
    EGFR-IN-139 (compound PD 18) is an epidermal growth factor receptor (EGFR) inhibitor, with IC50s of 12.88 (wild type), 10.84 (L858R/T790M), 42.68 (L858R/T790M/C797S) nM, respectively. EGFR-IN-139 displays strong anticancer activity against A549 and H1975 cancer cell lines, which are highly expressed EGFR. EGFR-IN-139 has a strong selectivity to cancer cells. EGFR-IN-139 can be used for nonsmall cell lung cancer (NSCLC) research[1].
    EGFR-IN-139
  • HY-172733S
    PRMT5-MTA-IN-3-d3

    		Isotope-Labeled Compounds Histone Methyltransferase Cancer
    PRMT5-MTA-IN-3-d3 (compound P22) is the deuterium labeled PRMT5-MTA-IN-3 (HY-172733). PRMT5-MTA-IN-3-d3 is an orally active PRMT5-MTA inhibitor. PRMT5-MTA-IN-3-d3 has antiproliferative effects on HTC116-MTAP del and wild type colorectal cancer HCT-116 cell lines, with IC50 values of 6 nM and 961 nM, respectively. PRMT5-MTA-IN-3-d3 has anticancer effects, especially for MTAP-deficient tumors, such as non-small cell lung cancer (NSCLC), pancreatic cancer .
    PRMT5-MTA-IN-3-d3
  • HY-179585
    DD-CIP2

    		Apoptosis Cancer
    DD-CIP2 is a DNA damage and apoptosis inducer. DD-CIP2 demonstrates effective anti-proliferative activity against multiple cancer cell. DD-CIP2 modulates the DNA damage response pathway, triggering robust DNA damage, cell cycle arrest, and apoptosis in vitro. DD-CIP2 demonstrates significant anti-tumor efficacy in vivo at well-tolerated doses, without substantial toxicity. DD-CIP2 exhibits superior cytotoxic potency against a broad panel of blood-and solid-tumor-derived cancer cell lines independent of their BRCA1/2 status. DD-CIP2 can be used for small-cell lung cancer (SCLC) and non small-cell lung cancer (NSCLC) research .
    DD-CIP2
  • HY-181890
    TRG-192

    		Glutaminase Cancer
    TRG-192 is a potent and selective glutaminase (GLS) inhibitor with an IC50 of 68 nM. TRG-192 inhibits intracellular glutamate levels. TRG-192 is applicable to related research on non-small cell lung cancer .
    TRG-192
  • HY-109061A
    Lazertinib mesylate hydrate

    YH25448 mesylate hydrate; GNS-1480 mesylate hydrate

    		 Apoptosis Akt TRP Channel EGFR ERK Cancer
    Lazertinib (YH25448; GNS-1480) mesylate hydrate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate hydrate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate hydrate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate hydrate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate hydrate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
    Lazertinib mesylate hydrate
  • HY-109061R
    Lazertinib (Standard)

    YH25448 (Standard); GNS-1480 (Standard)

    		 Apoptosis Akt TRP Channel EGFR ERK Reference Standards Infection Neurological Disease Metabolic Disease Cancer
    Lazertinib (Standard) is the analytical standard of Lazertinib (HY-109061). This product is intended for research and analytical applications. Lazertinib (YH25448) is a potent, selective, CNS-penetrant, orally available and irreversible EGFR tyrosine Kinase inhibitor, exhibiting high selectivity for activating (EGFRm) and T790M resistance mutations. Lazertinib inhibits phosphorylation of EGFR, AKT and ERK, leading to apoptosis and suppression of tumor growth in mouse H1975-luc brain metastasis xenograft models. Lazertinib can be used in the study of non-small cell lung cancer .
    Lazertinib (Standard)
  • HY-182264
    Masoprocol tetrapivalate

    Nordihydroguaiaretic acid tetrapivalate

    		 IGF-1R EGFR Drug Metabolite Cancer
    Masoprocol tetrapivalate (Nordihydroguaiaretic acid tetrapivalate) is a catecholic butane metabolite and also a tyrosine kinase activity inhibitor of IGF-1R and EGFR. Masoprocol tetrapivalate regulates tyrosine kinase signaling pathways associated with cell proliferation. Masoprocol tetrapivalate can be used in the research of proliferative diseases, including malignant, precancerous or benign cancers, and solid tumors .
    Masoprocol tetrapivalate

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