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Results for "

L858R/T790M

" in MedChemExpress (MCE) Product Catalog:

106

Inhibitors & Agonists

3

Isotope-Labeled Compounds

5

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-157398

    EGFR Cancer
    EGFR T790M/L858R-IN-3 (compound B1) is a EGFR L858R/T790M inhibitor with IC50 value of 13?nM. EGFR T790M/L858R-IN-3 shows anti-tumour activity in H1975 cells with an IC50 value of 0.087 μΜ. EGFR T790M/L858R-IN-3 inhibits cell migration in A549 cells and induces apoptosis in H1975 cells .
    EGFR <em>T790</em>M/<em>L858</em>R-IN-3
  • HY-162062

    EGFR Cancer
    EGFR WT/T790M/L858R-IN-1 (compound 10d) is a potent EGFR inhibitor, with IC50s of 0.097, 0.280, and 0.051?μM for EGFR WT, EGFR T790M, and EGFR L858R, respectively. EGFR WT/T790M/L858R-IN-1 can be used for the research of cancer .
    EGFR WT/<em>T790</em>M/<em>L858</em>R-IN-1
  • HY-142519

    EGFR Cancer
    EGFR-IN-27 is a potent EGFR inhibitor with IC50s of <50 nM for EGFR Del, L858R, Del/T790M, L858R/T790M, Del/T790M/C797S, and L858R/T790M/C797S, respectively (WO2021249324A1, compound 511) .
    EGFR-IN-27
  • HY-162299

    EGFR Cancer
    EGFR kinase inhibitor 3 (compound 2) is a bivalent ATP-allosteric EGFR kinase inhibitor with IC50s of <10 nM, 1.5 nM, 0.059 nM, 0.064 nM for WT EGFR, EGFR-activating mutations L858R, L858R/T790M and L858R/T790M/C797S, respectively. EGFR kinase inhibitor 3 is a C-linked inhibitor .
    EGFR kinase inhibitor 3
  • HY-142512

    EGFR Cancer
    EGFR-IN-24, a potent EGFR inhibitor, shows inhibition against EGFR(del19/T790M/C797S) and EGFR(L858R/T790M/C797S), respectively .
    EGFR-IN-24
  • HY-138072

    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-162254

    EGFR Ack1 Cancer
    EGFR T790M/L858R/ACK1-IN-1 is a dual inhibitor of EGFR T790M/L858R and ACK1. IC50 values are 23 and 263 nM, respectively. EGFR T790M/L858R/ACK1-IN-1 can inhibit cell proliferation and has antitumor activity .
    EGFR/ACK1-IN-1
  • HY-12026
    WZ4002
    5+ Cited Publications

    EGFR Cancer
    WZ4002 is a mutant selective EGFR inhibitor with IC50s of 2, 8, 3 and 2 nM for EGFR L858R, EGFR L858R/T790M, EGFR E746_A750 and EGFR E746_A750/T790M, respectively.
    WZ4002
  • HY-12001

    EGFR Cancer
    WZ3146 is a mutant selective EGFR inhibitor with IC50s of 2, 2, 5, 14 and 66 nM for EGFR L858R, EGFR L858R/T790M, EGFR E746_A750, EGFR E746_A750/T790M and EGFR, respectively.
    WZ-3146
  • HY-111415

    EGFR Cancer
    EGFR-IN-5 is a EGFR inhibitor with IC50s of 10.4, 1.1, 34, 7.2 nM for EGFR, EGFR L858R, EGFR L858R/T790M, and EGFR L858R/T790M/C797S, respectively.
    EGFR-IN-5
  • HY-10346
    AV-412
    2 Publications Verification

    MP412

    EGFR Cancer
    AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFR L858R, EGFR T790M, EGFR L858R/T790M and ErbB2, respectively.
    AV-412
  • HY-15772
    Osimertinib
    Maximum Cited Publications
    90 Publications Verification

    AZD-9291; Mereletinib

    EGFR Cancer
    Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
    Osimertinib
  • HY-15772A
    Osimertinib mesylate
    Maximum Cited Publications
    90 Publications Verification

    AZD-9291 mesylate; Mereletinib mesylate

    EGFR Cancer
    Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
    Osimertinib mesylate
  • HY-100213
    EAI045
    1 Publications Verification

    EGFR Cancer
    EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC50s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFR L858R, EGFR T790M and EGFR L858R/T790M at 10 μM ATP, respectively.
    EAI045
  • HY-10346A
    AV-412 free base
    2 Publications Verification

    MP-412 free base

    EGFR Cancer
    AV-412 free base (MP-412 free base) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFR L858R, EGFR T790M, EGFR L858R/T790M and ErbB2, respectively.
    AV-412 free base
  • HY-130608

    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-15772S

    AZD-9291-d6; Mereletinib-d6

    EGFR Cancer
    Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].
    Osimertinib-d6
  • HY-150610

    EGFR Cancer
    EGFR-IN-69 (compound 17g) is a potent EGFR inhibitor, with IC50 values of 4.3, 6.6 and 25.6 nM against EGFR L858R/T790M/C797S, EGFR L858R/T790M, and EGFR 19del/T790M/C797S, respectively. EGFR-IN-69 can be used for non-small-cell-lung-cancer (NSCLC) research .
    EGFR-IN-69
  • HY-146782

    EGFR Cancer
    EGFR-IN-49 is a potent and selective EGFR inhibitor with IC50s of 65.0 nM and 13.6 nM for EGFR T790M and EGFR T790M/L858R, respectively. EGFR-IN-49 induces late apoptosis in a dose-dependent manner .
    EGFR-IN-49
  • HY-155227

    Anaplastic lymphoma kinase (ALK) EGFR Apoptosis Cancer
    ALK/EGFR-IN-1 (Compound 8l) is an ALK/EGFR dual inhibitor that blocks the phosphorylation of EGFR and ALK. ALK/EGFR-IN-1 inhibits ALK/EGFR mutants respectively, with IC50 of 4.3 nM for EGFR L858R T790M in H1975 cells and EML4-ALK in BaF3 cells, respectively. and 3.6 nM. ALK/EGFR-IN-1 may be used in NSCLC research .
    ALK/EGFR-IN-1
  • HY-139920

    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-15164
    Icotinib Hydrochloride
    5+ Cited Publications

    BPI-2009H

    EGFR Cancer
    Icotinib Hydrochloride (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Icotinib Hydrochloride
  • HY-15164A
    Icotinib
    5+ Cited Publications

    BPI-2009

    EGFR Cancer
    Icotinib (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Icotinib
  • HY-12972

    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-128860

    EGFR Cancer
    Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=<1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity .
    Mutated EGFR-IN-2
  • HY-130616

    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-112823B
    Almonertinib hydrochloride
    3 Publications Verification

    HS-10296 hydrochloride

    EGFR Cancer
    Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib hydrochloride is used for the research of the non-small cell lung cancer .
    Almonertinib hydrochloride
  • HY-112823
    Almonertinib
    3 Publications Verification

    HS-10296

    EGFR Cancer
    Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .
    Almonertinib
  • HY-112823A
    Almonertinib mesylate
    3 Publications Verification

    HS-10296 mesylate

    EGFR Cancer
    Almonertinib (HS-10296) mesylate is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib mesylate is used for the research of the non-small cell lung cancer .
    Almonertinib mesylate
  • HY-19617A

    EGFR Cancer
    EGFR-IN-1 hydrochloride is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
    EGFR-IN-1 hydrochloride
  • HY-101450

    PF-6274484 is a potent EGFR inhibitor with Kis of 0.14 nM and 0.18 nM for EGFR-L858R/T790M and WT EGFR, respectively. PF-6274484 inhibits EGFR-L858R/T790M autophosphorylation in H1975 tumor cells and EGFR WT in A549 tumor cells with IC50s of 6.6 and 5.8 nM, respectively .
    PF-6274484
  • HY-146136

    EGFR Apoptosis Cancer
    EGFR-IN-56 (Compound 13a) is a potent EGFR inhibitor with IC50 values of 541.7 nM and 132.1 nM against EGFR T790M and EGFR T790M/L858R, respectively. EGFR-IN-56 blocks cancer cells in G2/M phase and induce into late apoptosis .
    EGFR-IN-56
  • HY-79077
    Osimertinib dimesylate
    Maximum Cited Publications
    90 Publications Verification

    AZD-9291 dimesylate; Mereletinib dimesylate

    EGFR Cancer
    Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFR L858R and EGFR L858R/T790M, respectively.
    Osimertinib dimesylate
  • HY-19617

    EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
    EGFR-IN-1
  • HY-19617B

    EGFR Cancer
    EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
    EGFR-IN-1 TFA
  • HY-135805

    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-78869

    Osimertinib analog

    EGFR Cancer
    Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant.
    Mutated EGFR-IN-1
  • HY-163094

    EGFR Cancer
    EGFR-IN-95 (compound 5j) is an 2,4-diaminonicotinamide derivative. EGFR-IN-95 has potent inhibitory activity against EGFR del19/T790M/C797S and L858R/T790M/C797S .
    EGFR-IN-95
  • HY-135914

    EGFR Cancer
    JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 15 nM for EGFR L858R/T790M .
    JBJ-02-112-05
  • HY-119944

    EGFR Cancer
    JND3229 is a reversible EGFR C797S inhibitor with IC50 values of 5.8, 6.8 and 30.5 nM for EGFR L858R/T790M/C797S, EGFR WT and EGFR L858R/T790M, respectively. JND3229 has good anti-proliferative activity and can effectively inhibit tumour growth in vivo. JND3229 can be used in cancer research, especially in non-small cell carcinoma .
    JND3229
  • HY-15164AS

    BPI-2009-d4

    Isotope-Labeled Compounds Others
    Icotinib-d4 is the deuterium-labeled Icotinib (HY-15164A). Icotinib-d4 (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib-d4 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Icotinib-d4
  • HY-161126

    EGFR Cancer
    EGFR-IN-98 (Compound 4c) is a EGFR inhibitor. The IC50 values of L858R/T790M/C797S and Del19/T790M/C797S are 0.277 μM and 0.089 μM, respectively. EGFR-IN 98 can be used in the study of tumors .
    EGFR-IN-98
  • HY-13984

    EGFR Cancer
    Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFR L858R, EGFR Exon 19 deletion and EGFR T790M.
    Mutant EGFR inhibitor
  • HY-157432

    EGFR Apoptosis Cancer
    EGFR-IN-97 (compound 6q) is a EGFR inhibitor. EGFR-IN-97 shows inhibitory activity against Ba/F3-EGFR L858R/T790M/C797S and Ba/F3-EGFR Del19/T790M/C797S cells, with IC50 values of 0.42 μM and 0.41 μM, respectively. EGFR-IN-97 can promote apoptosis of NCI-H1975-EGFR L858R/T790M/C797S cells at the concentration of 0.8 μM .
    EGFR-IN-97
  • HY-161319

    EGFR Cancer
    EGFR-IN-104 (Compound A23) is an effective inhibitor of EGFR, with IC50 values of 0.33 μM and 0.133 μM against EGFR L858R/T790M and EGFR Del19/T790M/C797S, respectively. EGFR-IN-104 exhibits anticancer activity both in vitro and in vivo .
    EGFR-IN-104
  • HY-161269

    EGFR Cancer
    EGFR-IN-101 (I-10) is a 2-phenylamino pyrimidine derivative. EGFR-IN-101 is a EGFR inhibitor. The IC50 values for EGFR L858R/T790M/C797S and Ba/F3-EGFR L858R/T790M/C797S are 33.26 and 106.4 nM, respectively. EGFR-IN-101 can be used IN the study of non-small cell lung cancer (NSCLC) .
    EGFR-IN-101
  • HY-151981

    EGFR Cancer
    EGFR-IN-74 (Compound 21) is a potent EGFR inhibitor with an IC50 of 138 nM against EGFR L858R/T790M. EGFR-IN-74 induces cancer cell apoptosis .
    EGFR-IN-74
  • HY-133780

    EGFR Autophagy Cancer
    Afatinib impurity 11 is an impurity of Afatinib. Afatinib is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively .
    Afatinib impurity 11
  • HY-161031

    EGFR Cancer
    EGFR-IN-93 (compound 18) is an allosteric inhibitor of T790M/L858R double mutant EGFR. EGFR-IN-93 can be used for non-small lung cancer (NSCLC) research .
    EGFR-IN-93
  • HY-15772S1

    AZD-9291-13C,d3; Mereletinib-13C,d3

    EGFR Cancer
    Osimertinib- 13C,d3 is the deuterium and 13C labeled Osimertinib. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively.
    Osimertinib-13C,d3

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