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Results for "

EGFR mutant non-small cell lung cancer

" in MedChemExpress (MCE) Product Catalog:

54

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1

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6

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Targets Recommended:
製品番号 製品名 Target 研究分野 構造式
  • 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-112870
    Firmonertinib
    Maximum Cited Publications
    6 Publications Verification

    Alflutinib; Furmonertinib; AST2818

    		 EGFR Cancer
    Firmonertinib (Alflutinib; Furmonertinib) is an orally active, mutant-selective, and highly brain penetrant EGFR inhibitor. Firmonertinib inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation .
    Firmonertinib
  • HY-400902
    VT3989

    		YAP VEGFR Hippo (MST) Cancer
    VT3989 is an orally active pan-TEAD autopalmitoylation inhibitor that modulates the Hippo signaling pathway. VT3989 directly binds to TEAD transcription factors to block their palmitoylation modification, thereby disrupting the formation of YAP/TAZ-TEAD complexes and inhibiting downstream oncogenic transcriptional activity. VT3989 effectively inhibits the growth of NF2-deficient schwannoma and meningioma cells and reverses the Schwann cell phenotype. In addition, VT3989 exerts a synergistic effect when combined with Osimtinib (HY-15772) in EGFR-mutant non-small cell lung cancer models, significantly delaying tumor recurrence and prolonging survival. VT3989 can be used for the research of epithelioid hemangioendothelioma, malignant pleural mesothelioma, type 2 neurofibromatosis and related advanced solid tumors .
    VT3989
  • HY-112870A
    Firmonertinib mesylate
    Maximum Cited Publications
    6 Publications Verification

    Alflutinib mesylate; Furmonertinib mesylate; AST2818 mesylate

    		 EGFR Inflammation/Immunology Cancer
    Firmonertinib (Alflutinib; Furmonertinib) mesylate is is an orally active, mutant-selective, and blood-brain barrier penetrant EGFR inhibitor. Firmonertinib mesylate inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib mesylate has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation .
    Firmonertinib mesylate
  • HY-13464
    ALK-IN-1

    Brigatinib analog

    		 Anaplastic lymphoma kinase (ALK) EGFR Cancer
    ALK-IN-1 is an orally active, blood-brain barrier-permeable ALK and EGFR inhibitor. ALK-IN-1 binds to and inhibits ALK kinase, ALK fusion proteins, and wild-type and mutant EGFR variants, thereby disrupting their corresponding signaling pathways. ALK-IN-1 can suppress the growth and proliferation of tumor cells and exhibits potential inhibitory activity against mutant EGFR. ALK-IN-1 can be used in the research of non-small-cell lung cancer .
    ALK-IN-1
  • HY-114358
    Tamnorzatinib
    2 Publications Verification

    ONO-7475

    		 TAM Receptor Trk Receptor Cancer
    Tamnorzatinib (ONO-7475) is a potent, selective, and orally active Axl/Mer inhibitor with IC50 values of 0.7 nM and 1.0 nM, respectively. Tamnorzatinib sensitizes AXL-overexpressing EGFR-mutant NSCLC cells to the EGFR-TKIs, suppresses the emergence and maintenance of tolerant cells. Tamnorzatinib combines with Osimertinib (HY-15772) provides a bright promise for the study of EGFR-mutated non-small cell lung cancer (NSCLC).
    Tamnorzatinib
  • HY-145574
    Iruplinalkib

    WX-0593

    		 Anaplastic lymphoma kinase (ALK) ROS Kinase BCRP Akt ERK STAT Cancer
    Iruplinalkib (WX-0593) is an orally active and selective ALK/ROS1 inhibitor. Iruplinalkib can effectively inhibit tyrosine autophosphorylation of ALK and mutant ALK, EGFR, with the IC50 between 5.38 and 16.74 nM. Iruplinalkib is also a suppressive agent of the transporter MATE1, MATE2K, P-gp and BCRP. Iruplinalkib can be used in the study of non-small cell lung cancer .
    Iruplinalkib
  • HY-109061B
    Lazertinib mesylate
    3 Publications Verification

    YH25448 mesylate; GNS-1480 mesylate

    		 TRP Channel EGFR Akt ERK Apoptosis Cancer
    Lazertinib (YH25448; GNS-1480) mesylate 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 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 induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate 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 is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
    Lazertinib mesylate
  • 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-134877
    BAY 2476568

    		EGFR ERK Akt Cancer
    BAY 2476568 is a potent and mutant-selective inhibitor targeting EGFR exon20 insertion variants. BAY 2476568 potently inhibits the kinase activity of EGFR exon20 insertion mutants (insASV, insSVD, insNPG) with IC50 values of 0.09 nM, 0.21 nM, and 0.11 nM, respectively. BAY 2476568 inhibits EGFR (Y1068) phosphorylation and reduces the phosphorylation of ERK1/2 and Akt (S473) in Ba/F3 cells expressing EGFR exon20 insertion mutants (insASV, insSVD). BAY 2476568 can be used for the study of non-small cell lung cancer (NSCLC) driven by EGFR exon20 insertion mutations .
    BAY 2476568
  • HY-12972
    Mavelertinib

    PF-06747775

    		 EGFR Cancer
    Mavelertinib is a selective, orally available and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC50s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC) .
    Mavelertinib
  • HY-139920
    Oritinib
    1 Publications Verification

    SH-1028

    		 EGFR Cancer
    Oritinib (SH-1028), an irreversible third-generation EGFR TKI, overcomes T790M-mediated resistance in non-small cell lung cancer. Oritinib (SH-1028), a mutant-selective inhibitor of EGFR kinase activity, inhibits EGFR WT, EGFR L858R, EGFR L861Q, EGFR L858R/T790M, EGFR d746-750 and EGFR d746-750/T790M kinases, with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM, respectively .
    Oritinib
  • HY-139997
    DDC-01-163

    		PROTACs EGFR Cancer
    DDC-01-163 is an allosteric PROTAC degrader targeting EGFR. DDC-01-163 is dependent on the ubiquitin–proteasome system. DDC-01-163 can selectively inhibit the proliferation of L858R/T790M (L/T) mutant Ba/F3 cells. DDC-01-163 is effective against Osimertinib (HY-15772)-resistant cells with L/T/C797S and L/T/L718Q EGFR mutations. DDC-01-163 exhibits enhanced anti-proliferative activity against L858R/T790M EGFR-Ba/F3 cells when combined with the ATP-site EGFR inhibitor Osimertinib. DDC-01-163 can be used for the study of non-small cell lung cancer .
    DDC-01-163
  • HY-W1123936B
    DBCO-PEG1000-FA

    DBCO-PEG1000-Folate

    		 Folate Receptor (FR) Cancer
    DBCO-PEG1000-FA (DBCO-PEG1000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .
    DBCO-PEG1000-FA
  • 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-W423595
    BEBT-109

    		EGFR Cancer
    BEBT-109 is a potent pan-mutant-selective EGFR inhibitor. BEBT-109 has improved pharmacokinetic properties. BEBT-109 can be used for multiple mutant-EGFR-driven non-small cell lung cancer (NSCLC) research .
    BEBT-109
  • HY-17654
    BIEGi-1

    		EGFR mTOR Cancer
    BIEGi-1 is an EGFR inhibitor. BIEGi-1 effectively disrupts the EGFR-Rheb interaction in cells. BIEGi-1 robustly inhibits EGFR kinase activity (reduces p-Y1068-EGFR) as well as mTORC1 activation (reduces p-T389-S6K1) in EGFR-mutant cells. BIEGi-1 shows strong antiproliferative effects on EGFR-mutant PC9 and HCC827 cells with IC50 values of 17 nM and 20 nM, respectively. BIEGi-1 can be used for the study of cancers harboring EGFR mutations, such as non-small cell lung cancer (NSCLC) .
    BIEGi-1
  • HY-123766
    EGFR-IN-99

    		EGFR Cancer
    EGFR-IN-99 (compound 1a) is a potent EGFR and HER2 Exon 20 insertion mutant inhibitor. EGFR-IN-99 has excellent antiproliferative activity against DFCI127 cells, with an EC50 of 11.5 nM. EGFR-IN-99 can be used for the research of non-small cell lung cancer (NSCLC) .
    EGFR-IN-99
  • 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-138072
    EMI1

    		EGFR Cancer
    EMI1 is an EGFR ex19del/T790M/C797S and EGFR L858R/T790M/C797S inhibitor. EMI1 can be used for the research of mutant EGFR-associated, drug-resistant non-small-cell lung cancer (NSCLC) .
    EMI1
  • HY-W1123936C
    DBCO-PEG2000-FA

    DBCO-PEG2000-Folate

    		 Folate Receptor (FR) Others
    DBCO-PEG2000-FA (DBCO-PEG2000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .
    DBCO-PEG2000-FA
  • HY-W1126467
    RAS-IN-5

    		Ras Cancer
    RAS-IN-5 (Example 2) is a RAS inhibitor. RAS-IN-5 significantly inhibits the interaction between RAF1 and active KRAS mutant protein or HRAS WT protein. RAS-IN-5 significantly inhibits the cell viability of KRAS, NRAS, and EGFR mutant cells. RAS-IN-5 can be used in the research of colorectal cancer, liver cancer, and non-small cell lung cancer .
    RAS-IN-5
  • HY-164056
    EGFR T790M/L858R-IN-8

    		EGFR Cancer
    EGFR T790M/L858R-IN-8 (Compound 9) is a selective EGFR T790M/L858R mutant kinase inhibitor with a IC50 of 56.8 μM, and it shows no inhibitory activity against wild-type EGFR. EGFR T790M/L858R-IN-8 can be used for the research of non-small cell lung cancer .
    EGFR T790M/L858R-IN-8
  • 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-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-164476
    ES-072

    		EGFR GSK-3 PD-1/PD-L1 Cancer
    ES-072 is an orally effective selective EGFR mutant (EGFR-T790M) inhibitor. ES-072 activates GSK3α by inhibiting EGFR-T790M activity, which promotes phosphorylation of PD-L1 at Ser279 and Ser283. The phosphorylated PD-L1 recruits the E3 ubiquitin ligase ARIH1, leading to ubiquitination and proteasomal degradation of PD-L1. This mechanism not only reduces cancer cell growth but also enhances anti-tumor immune response by lowering PD-L1 levels. ES-072 can be used to inhibit proliferation in non-small cell lung cancer (NSCLC) cells .
    ES-072
  • HY-178448
    EGFR-IN-178

    		EGFR JAK Ferroptosis Apoptosis Reactive Oxygen Species (ROS) Cannabinoid Receptor Glutathione Peroxidase Caspase Inflammation/Immunology Cancer
    EGFR-IN-178 is an orally active EGFR mutant inhibitor, exhibits highly selective inhibitory activity against mutants of the EGFR enzyme, including Del19 (IC50 = 3.4 nM), L858R/T790 M (IC50 = 2.9 nM), and Del19/T790 M (IC50 = 2.5 nM). EGFR-IN-178 has good activity against JAK2 (IC50 = 55.6 nM) and JAK3 (IC50 = 46.1 nM) kinases. EGFR-IN-178 can increase cellular lipid oxide MDA, meanwhile decrease GSH content, causing ferroptosis in cancer cells. EGFR-IN-178 promotes apoptosis by increasing cleaved caspase-3 expression. EGFR-IN-178 can inhibit the phosphorylation of EGFR protein and decrease the active form p-JAK2 for JAK2, induce an increase in intracellular ROS. EGFR-IN-178 can be used for the study of non-small cell lung cancer (NSCLC) .
    EGFR-IN-178
  • HY-161030
    EGFR-IN-92

    		EGFR Cancer
    EGFR-IN-92 (compound 15) is an allosteric T790M/L858R double mutant EGFR inhibitor. EGFR-IN-92 shows antiproliferative activity against H1975 non-small lung cancer (NSCLC) cancer cells expressing double mutant EGFR .
    EGFR-IN-92
  • HY-W1123936D
    DBCO-PEG3400-FA

    DBCO-PEG3400-Folate

    		 Folate Receptor (FR) Others
    DBCO-PEG-FA (DBCO-PEG-Folate) (MW 3400) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .
    DBCO-PEG3400-FA
  • HY-157526
    EGFR-TK-IN-1

    		EGFR Apoptosis Cancer
    EGFR-TK-IN-1 (compound 7o) is a potent mutant EGFR inhibitor with IC50 of 8.5 nM an 9.3 nM against EGFR L858R/T790M and EGFR Del19.EGFR-TK-IN-1 showes strong antiproliferative effects against EGFR mutant-driven non-small cell lung cancer (NSCLC) cells and induces cell apoptosis .
    EGFR-TK-IN-1
  • 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-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-142512
    EGFR-IN-24

    		EGFR Cancer
    EGFR-IN-24 is a selective EGFR triple mutant inhibitor with >300 nM IC50 against human EGFRdel19/T790M/C797S, EGFRL858R/T790M/C797S, and EGFRWT. EGFR-IN-24 can be used for the research of non-small cell lung cancer .
    EGFR-IN-24
  • HY-157166
    EGFR kinase inhibitor 2

    		EGFR Cancer
    EGFR kinase inhibitor 2 (compound A-7) is a potent EGFR inhibitor targeting EGFRL858R/T790M/C797S and EGFRDel19/T790M/C797S mutants. EGFR kinase inhibitor 2 has the potential to address acquired resistance in the treatment of non-small cell lung cancer .
    EGFR kinase inhibitor 2
  • HY-167948
    Dacomitinib metabolite M1/2

    		EGFR Cancer
    Dacomitinib metabolite M1/2 is a potent inhibitor of both wild-type (WT) EGFR and the T790M mutation, demonstrating significant activity against acquired resistance mechanisms in EGFR-mutant non-small-cell lung cancer (NSCLC).
    Dacomitinib metabolite M1/2
  • HY-170665
    EGFR T790M/L858R-IN-9

    		EGFR Cancer
    EGFR T790M/L858R-IN-9 (Compound 8) is an EGFR-L858R/T790M inhibitor that demonstrates potent inhibitory phosphorylation effects against the EGFR-L858R/T790M mutant kinase, with an IC50 value of 0.0064µM. EGFR T790M/L858R-IN-9 also inhibits the proliferation of non-small cell lung cancer (NSCLC) cells and can be utilized in cancer research .
    EGFR T790M/L858R-IN-9
  • HY-164464
    BPI-15086

    		EGFR Cancer
    BPI-15086 an orally active, potent, irreversible mutant-selective inhibitor of both EGFR and T790M resistance mutations tyrosine kinase. BPI-15086 can be used for the research of non-small-cell lung cancer .
    BPI-15086
  • HY-182742
    EGFR-IN-208

    		EGFR Cancer
    EGFR-IN-208 is an allosteric mutant EGFR L858R/T790M and EGFR L858R/T790M/C797S inhibitor, with IC50 values of 3.06 μM and 1.08 μM, respectively. EGFR-IN-208 binds to the allosteric site of EGFR and inhibits EGFR phosphorylation. EGFR-IN-208 induces apoptosis and exhibits antiproliferative effects in cancer cells. EGFR-IN-208 can be used in research related to non-small cell lung cancer .
    EGFR-IN-208
  • HY-175297
    EGFR T790M/VEGFR-2-IN-1

    		VEGFR EGFR Cancer
    EGFR T790M/VEGFR-2-IN-1 (Compound 6) is a dual EGFR T790M mutant (IC50=0.26 μM) and VEGFR-2 (IC50=0.95 μM) inhibitor. EGFR T790M/VEGFR-2-IN-1 blocks tumor cell proliferation and angiogenesis signaling pathways. EGFR T790M/VEGFR-2-IN-1 exhibits potent cytotoxicity against multiple cancer cell lines (HCT116, MCF-7, HepG2, A549; IC50=5.35-9.90 μM). EGFR T790M/VEGFR-2-IN-1 is promising for research of non-small cell lung cancer and solid tumors .
    EGFR T790M/VEGFR-2-IN-1
  • HY-13464R
    ALK-IN-1 (Standard)

    Brigatinib analog (Standard)

    		 Reference Standards Anaplastic lymphoma kinase (ALK) EGFR Cancer
    ALK-IN-1 (Standard) is the analytical standard of ALK-IN-1 (Brigatinib analog) (HY-13464). This product is intended for research and analytical applications. ALK-IN-1 is an ALK and EGFR inhibitor. ALK-IN-1 binds to and inhibits ALK kinase, ALK fusion proteins, and wild-type and mutant EGFR variants, thereby disrupting their corresponding signaling pathways. ALK-IN-1 can suppress the growth and proliferation of tumor cells and exhibits potential inhibitory activity against mutant EGFR. ALK-IN-1 can be used in the research of non-small-cell lung cancer .
    ALK-IN-1 (Standard)
  • HY-158988
    EGFR-IN-114

    		EGFR Cancer
    EGFR-IN-114 (Compound 241) is a non-covalent, selective mutant EGFR inhibitor. EGFR-IN-114 is applicable to the research of non-small cell lung cancer .
    EGFR-IN-114
  • HY-W1123936H
    DBCO-PEG10000-FA

    DBCO-PEG10000-Folate

    		 Folate Receptor (FR) Others
    DBCO-PEG10000-FA (DBCO-PEG10000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .
    DBCO-PEG10000-FA
  • HY-W1123936E
    DBCO-PEG5000-FA

    DBCO-PEG5000-Folate

    		 Folate Receptor (FR) Others
    DBCO-PEG5000-FA (DBCO-PEG5000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .
    DBCO-PEG5000-FA
  • HY-153605
    EGFR-IN-77

    		EGFR Cancer
    EGFR-IN-77 (Compound 4a) is a selective EGFR T790M/L858R inhibitor, with an IC50 of 0.101 μM against EGFR T790M/L858R, 0.477 μM against EGFR L858R, and 1.771 μM against wild-type EGFR. EGFR-IN-77 exerts selective antiproliferative effects on EGFR T790M/L858R non-small cell lung cancer. EGFR-IN-77 can be used for the research of EGFR L858R/T790M double-mutant non-small cell lung cancer .
    EGFR-IN-77
  • 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-182064
    EGFR-IN-206

    		EGFR NO Synthase COX NF-κB Interleukin Related Apoptosis Cancer
    EGFR-IN-206 is an orally active EGFR inhibitor. EGFR-IN-206 inhibits the phosphorylation of the key tumor growth protein EGFR, and suppresses the proliferation, migration and invasion of EGFR triple-mutant tumor cell lines. EGFR-IN-206 downregulates the expression of inflammation-related proteins iNOS, COX-2 and NF-κB (p65). EGFR-IN-206 promotes the secretion of NO. EGFR-IN-206 reduces the secretion of IL-6. EGFR-IN-206 induces apoptosis (apoptosis) of EGFR triple-mutant tumor cells. EGFR-IN-206 exerts antitumor activity in EGFR triple-mutant mice. EGFR-IN-206 is applicable to the research of non-small cell lung cancer .
    EGFR-IN-206
  • HY-112870AS
    Firmonertinib-d3 mesylate

    Alflutinib-d3 mesylate; Furmonertinib-d3 mesylate; AST2818-d3 mesylate

    		 Isotope-Labeled Compounds EGFR Inflammation/Immunology Cancer
    Firmonertinib-d3 (Alflutinib-d3) mesylate is the deuterium labeled Firmonertinib mesylate (HY-112870A). Firmonertinib (Alflutinib; Furmonertinib) mesylate is is an orally active, mutant-selective, and blood-brain barrier penetrant EGFR inhibitor. Firmonertinib mesylate inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib mesylate has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation.
    Firmonertinib-d3 mesylate
  • HY-180949
    EGFR-IN-189

    		EGFR ERK Cancer
    EGFR-IN-189 (Compound 7) is a selective covalent epidermal growth factor receptor (EGFR) inhibitor with an IC50 of 200 nM. EGFR-IN-189 can effectively inhibit the C797S mutant type of EGFR. EGFR-IN-189 can inhibit cancer cells proliferation and inhibit EGFR phosphorylation and downstream ERK1/2 phosphorylation. EGFR-IN-189 can be used for research of nonsmall cell lung cancer .
    EGFR-IN-189
  • HY-171884
    BI-8128

    		EGFR Cancer
    BI-8128 is a potent EGFR inhibitor, with IC50 values of 12, 6.7, 22, 10, and 3 nM against wild-type, T790M, C797S, T790M/C797S, and L858R/T790M/C797S mutant EGFR, respectively. BI-8128 significantly inhibits the proliferation of Ba/F3 and PC-9 drug-resistant mutant cells. BI-8128 is applicable for the research of non-small cell lung cancer .
    BI-8128
  • HY-180965
    Pro-PEG3-BA

    		PROTACs Anaplastic lymphoma kinase (ALK) EGFR Apoptosis Cancer
    Pro-PEG3-BA is an EML4-ALK/EGFR PROTAC degrader, degrading EML4 ALK and EGFR mutant (L858R/T790M) with DC 50 values of 0.42 and 13.50 μM, respectively. Pro-PEG3-BA hinders proliferation and induces cell cycle arrest and apoptosis of NSCLC cells in vitro. Pro-PEG3-BA shows safety profile and decreases EML4-ALK protein via rewiring the ubiquitin- proteasome system in vivo. Pro-PEG3-BA can be used for non-small cell lung cancer research .
    Pro-PEG3-BA

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