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EGFR (L858R/T790M/C797S mutant)

" in MedChemExpress (MCE) Product Catalog:
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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-135805
    JBJ-04-125-02

    		EGFR Cancer
    JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFR L858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFR L858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities .
    JBJ-04-125-02
  • HY-128862
    EGFR-IN-7

    		EGFR Cancer
    EGFR-IN-7 is a potent, selective and orally active EGFR kinase inhibitor. EGFR-IN-7 has inhibitory effect for for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) with IC50 values of 7.92 nM and 0.218 nM, respectively. EGFR-IN-7 can be used for the research of various cancers .
    EGFR-IN-7
  • HY-161536
    PROTAC EGFR degrader 9

    		PROTACs EGFR Apoptosis Cancer
    PROTAC EGFR degrader 9 (Compound C6) is an orally active CRBN-based PROTAC EGFR degrader. PROTAC EGFR degrader 9 exhibits a DC50 of 10.2 nM and a Kd of 240.2 nM against EGFR L858R/T790M/C797S. PROTAC EGFR degrader 9 exhibits potent degradation activity against various EGFR mutants, while sparing the EGFRWT. (Blue: CRBN ligand (HY-A0003), Black: linker (HY-161613); Pink: EGFR inhibitor (HY-161537)) .
    PROTAC EGFR degrader 9
  • 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-147183A
    JBJ-09-063 TFA

    		EGFR Cancer
    JBJ-09-063 TFA is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 TFA effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 TFA is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 TFA can be used for researching EGFR-mutant lung cancer .
    JBJ-09-063 TFA
  • HY-147183B
    JBJ-09-063 hydrochloride

    		EGFR Cancer
    JBJ-09-063 hydrochloride is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 hydrochloride effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 hydrochloride is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 hydrochloride can be used for researching EGFR-mutant lung cancer .
    JBJ-09-063 hydrochloride
  • HY-147183
    JBJ-09-063

    		EGFR Cancer
    JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer .
    JBJ-09-063
  • 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-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-130616
    EGFR-IN-11

    		EGFR Apoptosis Cancer
    EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFR L858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1 .
    EGFR-IN-11
  • HY-174826
    EGFR-IN-164

    		EGFR c-Kit Cancer
    EGFR-IN-164 (Compound 4) is a selective and covalent allosteric EGFR inhibitor. EGFR-IN-164 significantly inhibits the activity of EGFR L858R/T790M/C797S kinase (IC50: 48.1 nM) and proliferation of of EGFR-mutant cells. EGFR-IN-164 can be used for drug resistance of cancer research .
    EGFR-IN-164
  • 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-170497
    EGFR-IN-140

    		EGFR Cancer
    EGFR-IN-140 (Compound 31) is the inhibitor for EGFR, that inhibits EGFR wildtype and EGFR L858R/T790M/C797S mutant with Ki of 0.95 nM and 2.1 nM, and inhibits EGFR del19/T790M/C797S in Ba/F3 with an IC50 of 56.9 nM. EGFR-IN-140 exhibits antitumor efficacy in mouse model .
    EGFR-IN-140
  • HY-155005
    EGFR mutant-IN-2

    		EGFR Cancer
    EGFR mutant-IN-2 (Compound D51) is an EGFR mutant inhibitor. EGFR mutant-IN-2 inhibits the EGFR L858R/T790M/C797S mutant with an IC50 value of 14 nM. EGFR mutant-IN-2 inhibits the EGFR del19/T790M/C797S mutant with an IC50 value of 62 nM. EGFR mutant-IN-2 has favorable PK parameters, safety properties, in vivo stability, and antitumor activity .
    EGFR mutant-IN-2
  • HY-130608
    Mutated EGFR-IN-3

    		EGFR Cancer
    Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 values of 12 nM and 13 nM, respectively .
    Mutated EGFR-IN-3
  • HY-139884
    EGFR-IN-18

    		EGFR Cancer
    EGFR-IN-18 potently inhibits enzymatic activity in L858R/T790M/C797S mutant EGFR (4.9 nM), with a significantly lower activity for wild-type EGFR (47 nM).
    EGFR-IN-18
  • HY-164490
    LS-106

    		EGFR Apoptosis Cancer
    LS-106 is an orally active and potent inhibitor against epidermal growth factor receptor (EGFR) . LS-106 exhibits antitumor activities both in vitro and in vivo. LS-106 inhibits the kinase activities of EGFR 19del/T790M/C797S and EGFR L858R/T790M/C797S with IC50 values of 2.4 nmol/L and 3.1 nmol/L, respectively, which is more potent than Osimertinib (HY-15772). LS-106 induces Apoptosis, suppresses cell proliferation of tumor cells harboring EGFR 19del/T790M/C797S and leas to significant tumor regression in a C797S-mutant xenograft model .
    LS-106
  • HY-161785
    EGFR-IN-117

    		Apoptosis EGFR Cancer
    EGFR-IN-117 (Compound 8h) exhibits inhibitory activity against EGFR mutation, targets the tumor environment, and induces apoptosis of cancer cells. EGFR-IN-117 inhibits proliferations of H1975, PC-9, and EGFR mutant cells BaF3-EGFR L858R/T790M/C797S and BaF3– C797S/Del19/T790M, with IC50 of 13 nM, 19 nM, 1.2 nM and 1.3 nM, respectively. EGFR-IN-117 exhibits antitumor efficacy in mouse models .
    EGFR-IN-117
  • HY-125841
    EGFR mutant-IN-1

    		EGFR Cancer
    EGFR mutant-IN-1, a 5-methylpyrimidopyridone derivative, is a potent and selective EGFR L858R/T790M/C797S mutant inhibitor with an IC50 of 27.5 nM, while being a significantly less potent for EGFR WT (IC50 >1.0 μM) .
    EGFR mutant-IN-1
  • HY-161923
    EGFR-IN-120

    		EGFR Apoptosis Akt ERK Cancer
    EGFR-IN-120 (Compound 11eg) is an orally active EGFR inhibitor. EGFR-IN-120 inhibits EGFR L858R/T790M/C797S with an IC50 value of 0.053 μM, and has a relatively weak effect on EGFR WT (IC50: 1.05 μM). EGFR-IN-120 inhibits the phosphorylation of EGFR and main downstream effectors (STAT3, AKT, and Erk). EGFR-IN-120 induces cell cycle arrest and cell apoptosis in EGFR mutant cells. EGFR-IN-120 inhibits the proliferation of the NSCLC cells harboring EGFR L858R/T790M/C797S with an IC50 of 0.052 μM .
    EGFR-IN-120
  • HY-172780
    EGFR-IN-161

    		EGFR Apoptosis Cancer
    EGFR-IN-161 (Compound DD-8) is a potent and reversible inhibitor of L858R/T790M/C797S mutant EGFR kinases, with an IC50 of 0.87 nM. EGFR-IN-161 can induce apoptosis process, G1-phase arrestation, and migration inhibition in tumor cells .
    EGFR-IN-161
  • 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-E70700
    EGFR d746-750/T790M/C797S/L858R Recombinant Human Active Protein Kinase

    		EGFR Cancer
    EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR d746-750/T790M/C797S/L858R Recombinant Human Active Protein Kinase is a recombinant EGFR d746-750/T790M/C797S/L858R protein that can be used to study EGFR d746-750/T790M/C797S/L858R-related functions .
    EGFR d746-750/T790M/C797S/L858R Recombinant Human Active Protein Kinase
  • 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-181659
    EGFR-IN-201

    		EGFR Apoptosis Akt ERK Caspase Bcl-2 Family Cancer
    EGFR-IN-201 is a potent EGFR inhibitor, with an IC50 of 0.091 μM against wild-type EGFR; for mutant EGFR variants, the IC50 values of EGFR T790M, EGFR L858R and EGFR C797S are 0.147 μM, 0.221 μM and 0.703 μM, respectively. EGFR-IN-201 inhibits EGFR downstream signaling proteins AKT1 (IC50 = 0.225 μg/mL) and ERK1 (IC50 = 0.705 μg/mL). EGFR-IN-201 induces G0/G1 cell cycle arrest, apoptosis and low-level necrosis in cancer cells. EGFR-IN-201 is applicable to research on cancers such as colon cancer .
    EGFR-IN-201

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