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Isoforms Recommended: EGFR/ErbB1/HER1
Results for "

EGFRL858R

" in MedChemExpress (MCE) Product Catalog:

12

Inhibitors & Agonists

3

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15729
    Rociletinib
    Maximum Cited Publications
    13 Publications Verification

    CO-1686; AVL-301; CNX-419

    		 EGFR Cancer
    Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
    Rociletinib
  • HY-10261S1
    Afatinib-d4

    BIBW 2992-d4

    		 EGFR Autophagy Cancer
    Afatinib-d4 is the deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.
    Afatinib-d4
  • HY-10261AS
    Afatinib-d6 dimaleate

    BIBW 2992MA2-d6

    		 Isotope-Labeled Compounds EGFR Autophagy Cancer
    Afatinib-d6 (dimaleate) is the deuterium labeled Afatinib dimaleate. Afatinib dimaleate is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively[1][2].
    Afatinib-d6 dimaleate
  • HY-B0793S1
    AZ-5104-d2

    		EGFR Cancer
    AZ-5104-d2 is the deuterium labeled AZ-5104. AZ-5104 is an EGFR inhibitor with IC50s of 1 nM, 6 nM, 1 nM, 25 nM and 7 nM for EGFRL858R/T790M, EGFRL858R, EGFRL861Q, EGFR and ErbB4, respectively[1].
    AZ-5104-d2
  • HY-156457
    EGFR-IN-90

    		EGFR Cancer
    EGFR-IN-90 (compound 34) is an orally active EGFR inhibitor. EGFR-IN-90 shows inhibitory activity against EGFRL858R/T790M/C797S with an IC50 of 5.1 nM and inhibits the proliferation of the H1975-TM cell line harboring EGFRL858R/T790M/C797S with an IC50 of 0.05 μM. EGFR-IN-90 and inhibits tumor growth in the H1975-TM xenograft tumor model .
    <em>EGFR</em>-IN-90
  • HY-15729A
    Rociletinib hydrobromide
    Maximum Cited Publications
    13 Publications Verification

    CO-1686 hydrobromide; AVL-301 hydrobromide; CNX-419 hydrobromide

    		 EGFR Cancer
    Rociletinib hydrobromide (CO-1686 hydrobromide) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
    Rociletinib hydrobromide
  • HY-147858A
    PROTAC EGFR degrader 7 diTFA

    		PROTACs Cancer
    PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC50 of 13 .2 nM.PROTAC EGFR degrader 7 inhibits NCI-H1975 cells proliferation, with an IC50 of 46 .82 nM.PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI-H1975 cell.PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research .
    PROTAC <em>EGFR</em> degrader 7 diTFA
  • HY-155358
    Os30

    		EGFR Apoptosis Cancer
    Os30, a potent fourth-generation EGFR inhibitor, is a potent EGFRC797S-TK inhibitor with IC50 values of 18 nM and 113 nM for EGFRDel19/T790M/C797S TK and EGFRL858R/T790M/C797S TK, respectively. Os30 can suppress EGFR phosphorylation, arrest at G1 phase and induce the apoptosis of KC-0116 (BaF3-EGFRDel19/T790M/C797S) cells. Os30 shows potent antitumor efficacy on non-small cell lung cancer (NSCLC) with EGFmRC797S mutation .
    Os30
  • HY-12872
    Nazartinib
    5+ Cited Publications

    EGF816

    		 EGFR Cancer
    Nazartinib (EGF816) is a covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min −1 on EGFR(L858R/790M) mutant, respectively.
    Nazartinib
  • HY-12872A
    Nazartinib mesylate

    EGF816 mesylate

    		 EGFR Cancer
    Nazartinib mesylate (EGF816 mesylate) is a novel, covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min −1 on EGFR(L858R/790M) mutant, respectively.
    Nazartinib mesylate
  • HY-162062
    EGFR WT/T790M/L858R-IN-1

    		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 .
    <em>EGFR</em> WT/T790M/L<em>858</em>R-IN-1
  • HY-133780
    Afatinib impurity 11

    		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

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