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NSCLC xenografts

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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-P991669
    IGN523

    AML-01

    		 Caspase Apoptosis Cancer
    IGN523 is an anti-CD98 antibody (hCD98, KD = 0.55 nM). IGN523 induces antibody-dependent cell-mediated cytotoxicity (ADCC) activity, lysosomal membrane permeabilization, and inhibition of essential amino acid transport, ultimately leading to caspase-3 and caspase-7-mediated apoptosis of tumor cells. IGN523 inhibits tumor growth in multiple tumor xenograft models. IGN523 is useful in the research of non-small cell lung cancer (NSCLC), acute myeloid leukemia (AML), and other cancers. .
    IGN523
  • HY-153361
    YD23

    		PROTACs Epigenetic Reader Domain Inflammation/Immunology Cancer
    YD23 is a selective SMARCA2 PROTAC degrader with DC50 values of 64 nM and 297 nM in H1792 cells and H1975 cells. YD23 induces degradation of SMARCA2, which is synthetic lethal to SMARCA4. YD23 reduces chromatin accessibility only in SMARCA4 deficient cells, including cell cycle and cell growth regulatory genes. YD23 selectively inhibits growth of SMARCA4 mutant lung cancer cells. YD23 has potent tumor growth inhibitory activity in SMARCA4-mutant xenografts. YD23 can be used for the study of non-small cell lung cancer (NSCLC) .
    YD23
  • HY-148819A
    NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT hydrochloride

    		ADC Payload Topoisomerase Cancer
    NH2-bicyclopentane-7-MAD-MDCPT hydrochloride (Formula I) is a topoisomerase I (TOP1) inhibitor. NH2-bicyclopentane-7-MAD-MDCPT hydrochloride is applicable to the synthesis of the ADC ABBV-969. NH2-bicyclopentane-7-MAD-MDCPT hydrochloride is used in research on lung adenocarcinoma and melanoma .
    NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT hydrochloride
  • HY-175839
    PROTAC EGFR degrader 15

    		PROTACs EGFR ATP Synthase Cancer
    PROTAC EGFR degrader 15 is a Pomalidomide (HY-10984)-based Gefitinib (HY-50895) EGFR PROTAC degrader. PROTAC EGFR degrader 15 triggers EGFR degradation via ubiquitin-proteasome-dependent proteolysis and autophagy-lysosome activation pathways. PROTAC EGFR degrader 15 targets ETFA to enhance ATP production. PROTAC EGFR degrader 15 significantly suppresses tumor growth in a Gefitinib-acquired resistant HCC-827 xenograft model. PROTAC EGFR degrader 15 can be used for the study of non-small cell lung cancer (NSCLC) (Pink: EGFR ligand (HY-W109039); Blue: CRBN ligand (HY-10984); Black: Linker (HY-W679737)) .
    PROTAC EGFR degrader 15
  • HY-117366
    PS432

    		PKC Cancer
    PS432 is a PKC inhibitor with IC50s of 16.9 μM (PKCι) and 18.5 μM (PKCζ), respectively. PS432 effectively inhibits the proliferation of non-small cell lung cancer cells (NSCLCs) and tumor growth in mouse xenograft models .
    PS432
  • HY-161275
    BI-4732

    		EGFR Akt ERK Ribosomal S6 Kinase (RSK) Cancer
    BI-4732 is an orally active, reversible, ATP-competitive EGFR inhibitor with blood-brain barrier penetration. BI-4732 inhibits the kinase activity of EGFR L858R, T790M and C797S with IC50 values of 1 nM while sparing EGFR wild-type. BI-4732 inhibits EGFR and reduces the phosphorylation of AKT, ERK, and S6K. BI-4732 demonstrates excellent intracranial anti-tumor efficacy in YU-1097 xenograft model harboring EGFR_E19del/T790M/C797S. BI-4732 can be used for the study of non-small cell lung cancer (NSCLC) .
    BI-4732
  • HY-147259
    Dalmelitinib

    		c-Met/HGFR Cancer
    Dalmelitinib is an orally active selective c-Met kinase inhibitor (IC50: 2.9 nM) that binds to the ATP-binding region of c-Met. Dalmelitinib induces the phosphorylation of MET, partially or completely inhibits the phosphorylation of AKT and ERK. Dalmelitinib potently inhibits cancer cell (c-Met oncogene amplification) proliferation, and is used for the research of cancers like human non-small cell lung cancer (NSCLC) .
    Dalmelitinib
  • HY-P990947
    Tilatamig

    AZD9592 Antibody

    		 ADC Antibody EGFR Cancer
    Tilatamig (AZD9592 Antibody) is a human antibody of the Ig (G1-κ_G1-λ2) subtype that targets EGFR/MET. Tilatamig conjugates with the Top1 inhibitor AZ14170133 (HY-145399) to form the antibody-drug conjugate (ADC) Tilatamig samrotecan (HY-171124) (AZD9592). Tilatamig accurately targets NSCLC models including EGFR-mutant, EGFR-wildtype, and EGFR tyrosine kinase inhibitor-treated ones, and its activity correlates with high expression of EGFR, c-MET and SLFN11. Tilatamig is available for in vivo anti-tumor studies in patient-derived xenograft models of non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) .
    Tilatamig
  • HY-N7694
    Isotoosendanin
    1 Publications Verification

    		 TGF-β Receptor JAK STAT Apoptosis Inflammation/Immunology Cancer
    Isotoosendanin is an orally active TGFβR1 inhibitor and abrogating its kinase activity (IC50 = 6732 nM). Isotoosendanin inhibits the JAK/STAT3 signaling pathway by directly targeting SHP-2, enhancing its stability, and reducing its ubiquitination. Isotoosendanin inhibits TGF-β-induced reduces the migration, invasion, and metastasis in triple-negative breast cancer (TNBC) cells. Isotoosendanin exhibits anti-tumor efficacy in TNBC xenograft models and A549 xenograft tumors. Isotoosendanin exhibits significant anti-inflammatory effects in acetic acid-induced vascular permeability and λ-carrageenan-induced hind paw edema tests. Isotoosendanin can be used for the study of non-small cell lung cancer (NSCLC), TNBC and inflammation .
    Isotoosendanin
  • HY-151563A
    OTUB1/USP8-IN-1 TFA
    2 Publications Verification

    		 Deubiquitinase Cancer
    OTUB1/USP8-IN-1 TFA is the TFA salt form of OTUB1/USP8-IN-1 (HY-151563). OTUB1/USP8-IN-1 TFA is a dual inhibitor for OTUB1/USP8, IC50 for OTUB1 and USP8 is 0.17 and 0.28 nM, respectively. OTUB1/USP8-IN-1 TFA inhibits proliferation of NSCLC cells. OTUB1/USP8-IN-1 TFA exhibits good pharmacokinetic characters in ICR mouse, and exhibits antitumor activity in H1975 xenograft mouse model .
    OTUB1/USP8-IN-1 TFA
  • HY-145928B
    Divarasib adipate
    Maximum Cited Publications
    6 Publications Verification

    GDC-6036 adipate

    		 Ras Cancer
    Divarasib (GDC-6036) adipate is an orally active, selective KRASG12C inhibitor with an IC50 of <0.01 μM. Divarasib adipate covalently binds Cys12 in GDP-bound KRASG12C, occupies the switch II pocket, blocks GTP binding and SOS-mediated reactivation, and inhibits oncogenic KRAS signaling. Divarasib adipate induces tumor shrinkage and robust tumor growth inhibition in KRASG12C-positive models and cancer cells. Divarasib adipate can be used for the research of non-small cell lung cancer, colorectal adenocarcinoma, pancreatic ductal adenocarcinoma, and other KRASG12C-mutated solid tumors .
    Divarasib adipate
  • HY-158006
    SDX-7539

    		MetAP Cancer
    SDX-7539 is a selective inhibitor for Methionine aminopeptidase type 2 (MetAP2). SDX-7539 inhibits proliferarion of HUVECs with an IC50 of 120 μM. SDX-7539 exhibits antitumor activity in NSCLC xenograft athymic nude mice .
    SDX-7539
  • HY-124084
    SW203668

    		Stearoyl-CoA Desaturase (SCD) Cancer
    SW203668 is an irreversible stearoyl CoA desaturase (SCD) inhibitor with an IC50 of 54 nM. SW203668 covalently binds and inhibits SCD, depletes unsaturated fatty acids, and triggers cell death in sensitive cells. SW203668 requires demethylation by CYP4F11 to form its active SCD-inhibiting form; differential CYP4F11 expression drives selective cytotoxicity. SW203668 exerts cytotoxicity toward CYP4F11-expressing non-small cell lung cancer (NSCLC) cells and spares CYP4F11-lacking NSCLC cells. SW203668 inhibits tumor growth in immunodeficient mice bearing CYP4F11-expressing NSCLC xenografts and spares mouse skin sebocytes. SW203668 can be used for the research of non-small cell lung cancer .
    SW203668
  • HY-177445
    KAT6-IN-4

    		Histone Acetyltransferase Estrogen Receptor/ERR Cancer
    KAT6-IN-4 (Compound Example 2) is a selective lysine acetyltransferase 6 (KAT6) inhibitor. KAT6-IN-4 suppresses transcription of oncogenes like ERα. KAT6-IN-4 demonstrates potent antitumor efficacy in ER +/HER2 - breast cancer xenografts. KAT6-IN-4 is promising for research of KAT6-driven malignancies (e.g., breast cancer, NSCLC) .
    KAT6-IN-4
  • HY-174387
    KIN-8741

    		c-Met/HGFR Cancer
    KIN-8741 is a highly selective Type IIb c-Met inhibitor. KIN-8741 has broad activity against c-Met kinase mutations. KIN-8741 shows antitumor activity in MET gene amplified and exon 14 deleted non-small cell lung cancer models. KIN-8741 can be used in the research of c-Met driven cancers, especially advanced tumors carrying MET exon 14 jump mutations, acquired drug resistance mutations, etc .
    KIN-8741
  • HY-169061
    WQQ-345

    		Histone Methyltransferase Aminotransferases (Transaminases) Lactate Dehydrogenase Cancer
    WQQ-345 is an orally active BCAT1 inhibitor with an IC50 values of 10.8 mM. WQQ-345 reduces cellular α-KG levels, upregulating H3K27me3 expression, decreasing glycolytic enzyme expression, and impairing glycolysis activity. WQQ-345 reduces colony formation, suppresses growth of BCAT1-high TKI-resistant lung cancer cells. WQQ-345 exerts in vitro and in vivo antitumor activity. WQQ-345 can be used for the research of TKI-resistant non-small cell lung cancer and TKI-resistant lung cancer .
    WQQ-345
  • 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-179403
    KRASG12C IN-17

    		Ras Cancer
    KRASG12C IN-17 is an orally active covalent KRAS G12C inhibitor, showing strong inhibitory activity in KRAS G12C-mutant cancer cells (NCI-H23 IC50 = 0.7 nM; NCI-H358 IC50 = 0.5 nM). KRASG12C IN-17 covalently and irreversibly binds to KRAS G12C with > 96% modification efficiency in both GDP-bound and GMPPNP-bound conformations. KRASG12C IN-17 can be used for studies of KRAS-driven cancers, including colorectal cancer .
    KRASG12C IN-17
  • HY-130133
    DHW-221

    		PI3K mTOR Akt Apoptosis Paraptosis p38 MAPK Mitochondrial Metabolism P-glycoprotein CDK MMP HIF/HIF Prolyl-Hydroxylase VEGFR Cancer
    DHW-221 is a potent orally active dual PI3K/mTOR inhibitor, exhibiting low nanomolar potency against all four Class I PI3K isoforms and mTOR (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM; mTOR, IC50 = 3.9 nM). DHW-221 exerts antitumor effects by blocking the PI3K/Akt/mTOR pathway and inducing mitochondrial apoptosis and paraptosis (via Endoplasmic Reticulum (ER) stress and MAPK signaling) and arrests cell cycle, thereby inhibiting cell migration, invasion and angiogenesis. DHW-221 inhibits tumor growth in both the A549/Taxol (HY-B0015) and the HCC827 xenograft mouse models. DHW-221 can be used for non-small cell lung cancer (NSCLC), colon and breast cancer research .
    DHW-221
  • HY-175864
    EGFR-IN-173

    		EGFR Apoptosis p38 MAPK ERK Akt STAT Inflammation/Immunology Cancer
    EGFR-IN-173 is an orally active, pan-mutant EGFR tyrosine kinase inhibitor that targets EGFR 19del, L858R/T790M and C797S triple-mutations, potently inhibiting EGFR 19del/T790M/C797S with an IC50 of 1.19 nM while showing over 100-fold selectivity for mutant over wild-type EGFR (IC50 = 19.362 μM against WT). EGFR-IN-173 significantly inhibits cell migration, induces apoptosis in non-small cell lung cancer (NSCLC) cells. EGFR-IN-173 inhibits EGFR phosphorylation and suppresses the downstream pathways (MAPK/ERK, AKT, STAT3). EGFR-IN-173 exhibits antitumor efficacy in NSCLC and Ba/F3 xenograft models. EGFR-IN-173 can be used for NSCLC research .
    EGFR-IN-173
  • HY-124084A
    SW203668 TFA

    		Stearoyl-CoA Desaturase (SCD) Cancer
    SW203668 TFA is an irreversible stearoyl CoA desaturase (SCD) inhibitor with an IC50 of 54 nM. SW203668 TFA covalently binds and inhibits SCD, depletes unsaturated fatty acids, and triggers cell death in sensitive cells. SW203668 TFA requires demethylation by CYP4F11 to form its active SCD-inhibiting form; differential CYP4F11 expression drives selective cytotoxicity. SW203668 TFA exerts cytotoxicity toward CYP4F11-expressing non-small cell lung cancer (NSCLC) cells and spares CYP4F11-lacking NSCLC cells. SW203668 TFA inhibits tumor growth in immunodeficient mice bearing CYP4F11-expressing NSCLC xenografts and spares mouse skin sebocytes. SW203668 TFA can be used for the research of non-small cell lung cancer .
    SW203668 TFA
  • HY-174315
    WZH-17-002

    		PROTACs Anaplastic lymphoma kinase (ALK) Akt ERK Cancer
    WZH-17-002 is a WZH-15-125-based ALK PROTAC degrader with a DC50 of 25 nM. WZH-17-002 enhances activities against Lorlatinib (HY-12215)-resistant ALK compound mutations. WZH-17-002 significantly reduces drug resistance in ALK-fusion non-small cell lung cancer (NSCLC) and inhibits tumor growth in EML4-ALK G1202R/L1196 M xenograft mice model . Pink: ALK ligand (HY-174314); Blue: CRBN ligase ligand (HY-14658); Black: linker (HY-174316)
    WZH-17-002
  • HY-178391
    SMU-037

    		ROS Kinase p38 MAPK ERK Apoptosis Cancer
    SMU-037 is an orally active and selective ROS1 inhibitor that demonstrates potent activity (IC₅₀ = 6.8 nM) and possesses the ability to penetrate the blood-brain barrier. SMU-037 shows ~25-fold selectivity over ALK, and superior sensitivity against the G2032R mutation. SMU-037 attenuates phosphorylation of ROS1 and downstream MAPK-ERK signaling pathway, leading to cell cycle arrest and apoptosis. SMU-037 effectively suppresses tumor progression in both xenograft and intracranial mouse models. SMU-037 can be used for non-small cell lung cancer (NSCLC) research .
    SMU-037
  • HY-178008
    Mcl-1-IN-16

    		Bcl-2 Family Caspase Apoptosis Cancer
    Mcl-1-IN-16 is an effective macrocyclic myeloid cell leukemia 1 (Mcl-1) inhibitor with a Ki of below 0.08 nM. Mcl-1-IN-16 maintains high selectivity (>50,000-fold) for Mcl-1 over other antiapoptotic Bcl-2 family members Bcl-2 and Bcl-xL. Mcl-1-IN-16 leads to the activation of caspase-3/7, thereby initiating cell apoptosis. Mcl-1-IN-16 achieves tumor regression in a lung cancer-derived tumor xenograft mice model. Mcl-1-IN-16 can be used in the research of solid tumor such as nonsmall cell lung cancer (NSCLC) .
    Mcl-1-IN-16
  • HY-175527
    ALK degrader 2

    		HyT Anaplastic lymphoma kinase (ALK) Apoptosis Inflammation/Immunology Cancer
    ALK degrader 2 is an orally active ALK HyT degrader that degrades EML4-ALK levels (DC50 = 8 nM) and nucleophosmin (NPM)-ALK protein levels (DC50 = 102 nM). ALK degrader 2 mediates ALK degradation via the Hsp70 chaperone system and ubiquitin-proteasome pathway. ALK degrader 2 induces significant S-phase cell cycle arrest and apoptosis in H3122 cells. ALK degrader 2 shows anti-tumor activity in mice bearing H3122 xenografts. ALK degrader 2 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: ALK ligand (HY-W754809), Blue: Hyt (HY-W013021), Black: Linker (HY-Y1760), ALK ligand-linker conjugate (HY-175528)) .
    ALK degrader 2
  • 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-177021
    Tubulin-IN-51

    		Microtubule/Tubulin Apoptosis Cancer
    Tubulin-IN-51 is an orally available, potent tubulin inhibitor (IC50 = 31 nM). Tubulin-IN-51 promotes tubulin polymerization in vitro and does not compete with Paclitaxel (HY-B0015) for binding. Tubulin-IN-51 inhibits the binding of Vinblastine (HY-13780) to tubulin. Tubulin-IN-51 downregulates the proportion of cells in the G1 phase and induces apoptosis. Tubulin-IN-51 inhibits tumor growth in multiple nude mouse xenograft models .
    Tubulin-IN-51
  • HY-175206
    P-gp-IN-30

    		P-glycoprotein Cancer
    P-gp-IN-30 (Compound 13) is a P-glycoprotein (P-gp) inhibitor by targeting YB-1. P-gp-IN-30 significantly enhances sensitivity to Paclitaxel by reducing total YB-1 and nucleus YB-1 protein expression, inhibiting the expression and function of downstream P-gp, further suppressing the efflux rate of Paclitaxel. P-gp-IN-30 potently inhibits tumor growth in A549/Taxol xenografts mice model with combination of Paclitaxel (HY-B0015). P-gp-IN-30 can be used for non-small cell lung cancer (NSCLC) research .
    P-gp-IN-30
  • HY-123020
    CYD-2-88

    BDA-366 analog

    		 Bcl-2 Family Cancer
    CYD-2-88 (BDA-366 analog) is a BDA-366 (HY-101083) (Bcl2 BH4 antagonist) analog. CYD-2-88 (20 mg/kg, i.p.) inhibits tumor growth in NSCLC H460 xenografts mice .
    CYD-2-88
  • HY-149352
    DG1

    		Thymidylate Synthase Cancer
    DG1 (Compound 8Nc) is a Thymidylate Synthase (TS) inhibitor that affects cancer angiogenesis and metabolic reprogramming in NSCLC cells. DG1 can effectively inhibit the expression of CD26, ET-1, FGF-1 and EGF. DG1 also effectively inhibits the proliferation of cancer tissue in the A549 xenograft mouse model .
    DG1
  • HY-147994
    EGFR/HER2-IN-5

    		EGFR Cancer
    EGFR/HER2-IN-5 (compound 6h) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-5 inhibits EGFR with an IC50 value of 1.01 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-5 has potent antitumor efficacy in vivo and can be used for lung cancer research .
    EGFR/HER2-IN-5
  • HY-147992
    EGFR/HER2-IN-4

    		EGFR Cancer
    EGFR/HER2-IN-4(compound 6d) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-4 inhibits EGFR with an IC50 value of 0.6 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-4 has potent antitumor efficacy in vivo and can be used for lung cancer research .
    EGFR/HER2-IN-4
  • HY-173065
    CDK9-IN-36

    		CDK Apoptosis Cancer
    CDK9-IN-36 (Compound T7) is a potent, selective and metabolically stable CDK9 inhibitor with an IC50 value of 1.2 nM. CDK9-IN-36 effectively suppresses cell proliferation, reduces colony formation, and induces apoptosis in Osimertinib (HY-15772)-resistant NSCLC cells by downregulating Mcl-1. CDK9-IN-36 also demonstrates antitumor efficacy in a tumor xenograft model .
    CDK9-IN-36
  • HY-149695
    EGFR-IN-91

    		EGFR Cancer
    EGFR-IN-91 (compound 9) is an orally available EGFR inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFR L858R/C797S and EGFR exon 19del/C797S, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants .
    EGFR-IN-91
  • 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-114253
    ODS-2004436

    		EGFR Cancer
    ODS-2004436 is a small molecule radiotracer that uses positron emission tomography (PET) imaging to measure the activity of the epidermal growth factor receptor (EGFR) in tumors. ODS-2004436 labeled with the radioactive isotope fluorine-18 shows significantly higher uptake in the xenograft models of lung cancer with EGFR mutations compared to the wild-type models, and could be used to distinguish the mutation status. ODS-2004436 can be used to identify EGFR-positive tumors and predict their response to certain reagent treatments, especially for non-small cell lung cancer (NSCLC) .
    ODS-2004436
  • HY-W110138
    Chloroxoquinoline

    		DNA/RNA Synthesis Cytochrome P450 ROCK Cancer
    Chloroxoquinoline is an anticancer agent. Chloroxoquinoline damages the DNA templates of cancer cells, inducing DNA breaks and cell death, and inhibits cell invasion via down-regulating Rho/Rho kinase signaling pathway. Chloroxoquinoline enhances the radiation sensitivity of Lewis lung cancer cells and xenograft tumors in tumor-bearing mouse models but decreases efficacy after long term exposure in rat models by auto-induction effects on CYP1A and CYP3A. Chloroxoquinoline has a broad-spectrum anticancer activity, such as non-small-cell lung carcinoma (NSCLC), breast cancer and gastric cancer .
    Chloroxoquinoline
  • HY-168893
    K882

    		Src Apoptosis IAP Survivin Akt mTOR JAK STAT Ras p38 MAPK Cancer
    K882 (Compound 4e) is a Src inhibitor, with KD of 0.315 μM. K882 induces Apoptosis. K882 inhibits XIAP and Survivin. K882 inhibits the activation of PI3K/Akt/mTOR, Jak1/Stat3, Ras/MAPK signaling pathways. K882 shows anti-tumor activity against non-small cell lung cancer .
    K882
  • HY-176942
    JYP0322

    ROS1-IN-3

    		 ROS Kinase Trk Receptor Cancer
    YP0322 (ROS1-IN-3) is a potent orally active, selective, and CNS-penetrant ROS1 inhibitor. JYP0322 selectively inhibits human wild-type ROS1 and human ROS1 G2032R with IC50s of 0.37 and 0.3 nM, respectively, showing 6-130-fold selectivity over TRKA, TRKB, and TRKC. JYP0322 inhibits proliferation of ROS1 fusion-expressing cells, and inhibits tumor growth in mouse xenograft models. JYP0322 can be used for the research of non-small cell lung cancer (NSCLC) .
    JYP0322
  • HY-178451
    NQO1-responsive prodrug

    		Apoptosis Cancer
    NQO1-responsive prodrug is a prodrug of Gemcitabine (dFdC) (HY-17026) with anti-cancer effect. NQO1-responsive prodrug remains stable in plasma and liver/intestinal S9 fractions, releasing dFdC in an NQO1-dependent manner. NQO1-responsive prodrug induces S-phase arrest and apoptosis. NQO1-responsive prodrug inhibits tumor growth in an A549 xenograft mouse model. NQO1-responsive prodrug can be used for breast and non-small cell lung cancer (NSCLC) research .
    NQO1-responsive prodrug
  • HY-150774
    HDAC6/HSP90-IN-2

    		HDAC HSP Apoptosis Cancer
    HDAC6/HSP90-IN-2 (compound 6e) is a dual inhibitor of HDAC6 and Hsp90, with IC50s of 105.7 and 61 nM, respectively. HDAC6/HSP90-IN-2 can be used for the research of cancer .
    HDAC6/HSP90-IN-2
  • HY-170968
    EGFR-IN-150

    		EGFR Apoptosis Cancer
    EGFR-IN-150 is an EGFR inhibitor that effectively suppresses the phosphorylation of mutant epidermal growth factor receptor (EGFR) and its downstream AKT signaling pathway, thereby exerting antitumor effects and inducing HMOX1 expression to trigger ferroptosis. EGFR-IN-150 exhibits an IC50 of 0.386 μM against the non-small cell lung cancer (NSCLC) cell line H1975, and significantly inhibits colony formation and migration of both H1975 and A549 cells while inducing apoptosis. In addition, EGFR-IN-150 markedly suppresses tumor growth in the H1975 cell-derived xenograft (CDX) mouse model. EGFR-IN-150 holds promise for research related to non-small cell lung cancer .
    EGFR-IN-150
  • HY-171509
    Mal-N(Me)-C6-N(Me)-PNU-159682

    		Drug-Linker Conjugates for ADC Apoptosis Cancer
    Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27), an agent-linker conjugate for ADC, consists the ADC linker Mal-N(Me)-C6-N(Me) and a potent ADC cytotoxin PNU-159682. Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27) selectively delivers the payload to CD46-expressing cells, where the linker is cleaved by cathepsin B to release PNU-159682, inducing DNA damage and apoptosis. Mal-N(Me)-C6-N(Me)-PNU-159682 shows durable tumor regression in xenograft (PDX) models of non-small cell lung cancer (NSCLC) and colorectal cancer (CRC) .
    Mal-N(Me)-C6-N(Me)-PNU-159682
  • HY-180241
    Glutaminase C-IN-3

    		Glutaminase Reactive Oxygen Species (ROS) Cancer
    Glutaminase C-IN-3 is a potent allosteric inhibitor of Glutaminase C (GAC) with an EC50 of 116 nM. Glutaminase C-IN-3 regulates cellular metabolites and increases reactive oxygen species (ROS) production by blocking glutamine metabolism. Glutaminase C-IN-3 exhibits strong antitumor activity in an A549 xenograft mouse model. Glutaminase C-IN-3 can be used for the research of non-small cell lung cancer (NSCLC) .
    Glutaminase C-IN-3
  • HY-180430
    Antitumor agent-208

    		Drug Derivative Cancer
    Antitumor agent-208, a Bufalin (HY-N0877) analogue, is a potent and orally active antitumor agent. Antitumor agent-208 exhibits antiproliferative activity against tumor cell line (IC50 =0.30-1.09 nM). Antitumor agent-208 inhibits tumor growth in a MV-4-11 xenograft mouse model. Antitumor agent-208 can be used for cancer research, such as acute myeloid leukemia (AML) and non-small cell lung cancer (NSCLC) .
    Antitumor agent-208
  • HY-182914
    NGI-189

    		EGFR Akt Bcl-2 Family Apoptosis Cancer
    NGI‑189 is a selective OST‑A inhibitor. NGI‑189 inhibits the STT3A catalytic subunit of the OST complex and reduces N‑glycosylation of target glycoproteins. NGI‑189 blocks oncogenic and bypass signaling, reduces phosphorylation of EGFR, AKT, p70S6K and S6RP, and induces cell cycle arrest and apoptosis. NGI‑189 markedly suppresses tumor growth and induces tumor regression in non‑small cell lung cancer (NSCLC) xenograft models. NGI‑189 can be used for the research of EGFR‑mutant non‑small cell lung cancer .
    NGI-189
  • HY-182672
    VT101

    		YAP Cancer
    VT101 is a TEAD inhibitor with an IC50 of 454 nM. VT101 is applicable for cancer research .
    VT101
  • 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)

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