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EGFR degrader

" in MedChemExpress (MCE) Product Catalog:

41

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4

Inhibitory Antibodies

1

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Click Chemistry

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-146349
    PROTAC EGFR degrader 4

    		PROTACs EGFR Autophagy Cancer
    PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant EGFR.PROTAC EGFR degrader 4 induces EGFR del19 and EGFR L858R/T790M degradation with DC50s of 0.51 and 126 nM, respectively. PROTAC EGFR degrader 4 significantly inhibits growth of HCC827 and H1975 cell lines with IC50s of 0.83 and 203.1 nM, respectively. Induced EGFR degradation is related to autophagy .
    PROTAC EGFR degrader 4
  • HY-144605
    PROTAC EGFR degrader 3

    		EGFR PROTACs Cancer
    PROTAC EGFR degrader 3 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 3 shows excellent cellular activity against the H1975 and HCC827 cells with high selectively. PROTAC EGFR degrader 3 shows that the lysosome is involved in the degradation process of EGFR mutant degradation .
    PROTAC EGFR degrader 3
  • HY-144304
    PROTAC EGFR degrader 2

    		PROTACs EGFR Cancer
    PROTAC EGFR degrader 2 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 2 exhibits excellent antiproliferative activity with IC50 of 4.0 nM and good EGFR degradation activity with DC50 of 36.51 nM. PROTAC EGFR degrader 2 can be used for the synthesis of nitroreductase (NTR)-responsive PROTAC .
    PROTAC EGFR degrader 2
  • HY-153901
    PROTAC EGFR degrader 8

    		EGFR PROTACs Cancer
    PROTAC EGFR degrader 8 (T-184) is a PROTAC EGFR degrader. PROTAC EGFR degrader 8 degrades EGFR in HCC827 cell with a DC50 of 15.56 nM. PROTAC EGFR degrader 8 inhibits H1975, PC-9, HCC827 cell growth with IC50s of 7.72 nM, 121.9 nM, 14.21 nM. PROTAC EGFR degrader 8 can be used for research of cancer, especially NSCLC .
    PROTAC EGFR degrader 8
  • HY-147858
    PROTAC EGFR degrader 7

    		PROTACs EGFR Apoptosis Cancer
    PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR L858R/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 EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    PROTAC EGFR degrader 7
  • HY-161633
    PROTAC EGFR degrader 11

    		PROTACs EGFR FAK Cancer
    PROTAC EGFR degrader 11 (Compound B71) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC50 <100 nM. PROTAC EGFR degrader 11 binds CRBN-DDB1 with a Ki of 36 nM. PROTAC EGFR degrader 11 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC50 <100 nM.
    PROTAC EGFR degrader 11
  • HY-161632
    PROTAC EGFR degrader 10

    		PROTACs EGFR FAK Cancer
    PROTAC EGFR degrader 10 (Compound B56) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC50 <100 nM. PROTAC EGFR degrader 10 binds CRBN-DDB1 with a Ki of 37 nM. PROTAC EGFR degrader 10 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC50 <150 nM .
    PROTAC EGFR degrader 10
  • HY-146423
    PROTAC EGFR degrader 6

    		PROTACs EGFR Apoptosis Cancer
    PROTAC EGFR degrader 6, a PROTAC EGFR degrader, potently degrades EGFR Del19 in HCC827 cells with the DC50 of 45.2 nM. PROTAC EGFR degrader 6 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase .
    PROTAC EGFR degrader 6
  • HY-146422
    PROTAC EGFR degrader 5

    		PROTACs EGFR Apoptosis Cancer
    PROTAC EGFR degrader 5 (Compound 10), a PROTAC EGFR degrader, potently degrades EGFR Del19 in HCC827 cells with the DC50 of 34.8 nM. PROTAC EGFR degrader 5 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase .
    PROTAC EGFR degrader 5
  • 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-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 EGFR degrader 7 diTFA
  • HY-141640
    MS154

    		PROTACs EGFR Cancer
    MS154 is a first-in-class E3 ligase cereblon-recruiting EGFR degrader with Kds of 1.8 nM and 3.8 nM for EGFR WT and EGFR L858R mutants. MS154 potently inhibits cell proliferation in lung cancer cells .
    MS154
  • HY-157582
    MS39N

    		EGFR Others
    MS39N (compound 27) is a negative control for MS39 that binds EGFR without inducing degradation .
    MS39N
  • HY-131865
    SJF-1521

    		PROTACs EGFR Others
    SJF-1521 is a selective EGFR PROTAC degrader. SJF-1521 contains the EGFR inhibitor lapatinib (HY-50898). SJF-1521 can induce EGFR degradation in OVCAR8 cells .
    SJF-1521
  • HY-141486A
    PROTAC PARP/EGFR ligand 1

    		PARP EGFR Ligands for Target Protein for PROTAC Others
    PROTAC PARP/EGFR ligand 1 is an active compound that can be used for the synthesis of dual PARP EGFR degraders by proteolytic targeting chimera (PROTAC) technology .
    PROTAC PARP/EGFR ligand 1
  • HY-P99406
    Petosemtamab

    MCLA 158

    		 EGFR Cancer
    Petosemtamab (MCLA 158) is an anti- EGFR (Kd: 0.22 nM) and anti-LGR5 (Kd: 0.86 nM) monoclonal antibody (mAb). Petosemtamab leads to EGFR signaling blockade and receptor degradation in LGR5+ cancer cells. Petosemtamab can be used in the research of solid tumors, such as head and neck squamous cell carcinoma (HNSCC), metastatic colorectal cancer (CRC) .
    Petosemtamab
  • HY-161537
    EGFR ligand-9

    		EGFR Cancer
    EGFR ligand-9 is an EGFR ligand. EGFR ligand-9 can be used for synthesis of PROTAC EGFR degrader 9 (HY-161536) .
    EGFR ligand-9
  • HY-147942
    MS9449

    		PROTACs EGFR Cancer
    MS9449 is a potent PROTAC EGFR degrader with Kds of 17 nM and 10 nM for EGFR WT and EGFR L858R, respectively. MS9449 effectively induces degradation of mutant EGFRs through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9449 potently inhibits the proliferation of NSCLC cells. MS9449 can be used for researching anticancer .
    MS9449
  • HY-147941
    MS9427

    		PROTACs EGFR Cancer
    MS9427 is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer .
    MS9427
  • HY-147941A
    MS9427 TFA

    		PROTACs EGFR Cancer
    MS9427 TFA is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 TFA selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 TFA potently inhibits the proliferation of NSCLC cells. MS9427 TFA can be used for researching anticancer .
    MS9427 TFA
  • HY-161613
    7-Bromoheptanoyl chloride

    		PROTAC Linkers Cancer
    7-Bromoheptanoyl chloride is a linker of PROTAC EGFR degrader 9 (HY-161536) .
    7-Bromoheptanoyl chloride
  • HY-141481
    DP-C-4

    		PROTACs EGFR PARP Cancer
    DP-C-4 is a Cereblon-based dual PROTAC for simultaneous degradation of EGFR and PARP .
    DP-C-4
  • HY-141486
    (Rac)-PROTAC PARP/EGFR ligand 1

    		Target Protein Ligand-Linker Conjugates Cancer
    (Rac)-PROTAC PARP/EGFR ligand 1 incorporates a ligand for PARP and EGFR , and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). (Rac)-PROTAC PARP/EGFR ligand 1 can be used in the synthesis of DP-C-4, which is CRBN-based dual PROTAC for simultaneous degradation of EGFR and PARP .
    (Rac)-PROTAC PARP/EGFR ligand 1
  • HY-133110
    Afatinib N-Oxide

    		Drug Metabolite Others
    Afatinib N-Oxide is an impurity of Afatinib dimaleate in oxidative degradation. Afatinib dimaleate is an irreversible EGFR family inhibitor .
    Afatinib N-Oxide
  • HY-139997
    DDC-01-163

    		PROTACs EGFR Cancer
    DDC-01-163 is a mutant-selective allosteric PROTAC-based EGFR degrader, with an IC50 of 45 nM (Pink: EGFR ligand (HY-151048); Black: linker (HY-W008005); Blue: CRBN ligand (HY-14658)) .
    DDC-01-163
  • HY-N1166
    Tephrosin
    2 Publications Verification

    Deguelinol I; Hydroxydeguelin

    		 EGFR Cancer
    Tephrosin is a natural rotenoid which has potent antitumor activities. Tephrosin induces degradation of of EGFR and ErbB2 by inducing internalization of the receptors .
    Tephrosin
  • HY-131864
    SJF-1528

    		EGFR PROTACs Cancer
    SJF-1528 is a potent EGFR PROTAC degrader with DC50 values of 39.2 nM and 736.2 nM for wild-type EGFR in OVCAR8 cells and Exon 20 Ins mutated EGFR in HeLa cells. SJF-1528 also degrades HER2 (Pink: ligand for target protein (HY-159047); Black: linker Tos-PEG2-CH2-Boc (HY-130532); Blue: ligand for E3 ligase (S,R,S)-AHPC (HY-125845)) .
    SJF-1528
  • HY-131864A
    SJF-1528 hemihydrate

    		PROTACs EGFR Cancer
    SJF-1528 hemihydrate is the hemihydrate form of SJF-1528 (HY-131864). SJF-1528 hemihydrate is a EGFR PROTAC degrader with DC50 values of 39.2 nM and 736.2 nM for wild-type EGFR in OVCAR8 cells and Exon 20 Ins mutated EGFR in HeLa cells. SJF-1528 hemihydrate also degrades HER2. (Pink: ligand for target protein (HY-159047); Black: linker Tos-PEG2-CH2-Boc (HY-130532); Blue: ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
    SJF-1528 hemihydrate
  • HY-123921
    Gefitinib-based PROTAC 3
    3 Publications Verification

    		 PROTACs EGFR Cancer
    Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a von Hippel-Lindau ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively .
    Gefitinib-based PROTAC 3
  • HY-130549
    Acid-PEG3-C2-Boc

    		PROTAC Linkers Cancer
    Acid-PEG3-C2-Boc is a PEG- and Alkyl/ether-based PROTAC linker can be used in the synthesis of PROTACs for the degradation of EGFR and inhibition of mTOR .
    Acid-PEG3-C2-Boc
  • HY-161538
    Lenalidomide-C6-Br

    		E3 Ligase Ligand-Linker Conjugates Cancer
    Lenalidomide-C6-Br is a conjugate of E3 ligase ligand and linker. Lenalidomide-C6-Br can be utilized for synthesis of PROTAC EGFR degrader 9 (HY-161536) .
    Lenalidomide-C6-Br
  • HY-164548
    WK88-1

    		HSP Apoptosis Cancer
    WK88-1, a Hsp90 inhibitor, induces overall degradation of multiple oncogenic signaling molecules including EGFR, ErbB2 and ErbB3, leading to subsequent growth arrest and apoptosis in the Gefitinib-resistant H1975 cell line .
    WK88-1
  • HY-P9977
    Amivantamab
    1 Publications Verification

    JNJ-61186372

    		 EGFR Cancer
    Amivantamab (JNJ-61186372) is a human EGFR-MET bispecific antibody with immune anticancer activity. Amivantamab inhibits ligand binding, promotes endocytosis and degradation of receptor-antibody complexes, and induces Fc-dependent cytokinesis in macrophages and antibody-dependent cytotoxicity in natural killer cells .
    Amivantamab
  • HY-P99406A
    Petosemtamab (FUT8-KO)

    		EGFR Cancer
    Petosemtamab (FUT8-KO) is a knockout version of petosemtamab for the fucosyltransferase 8 gene (FUT8). Petosemtamab (HY-P99406) is an anti-EGFR (Kd: 0.22 nM) and anti-LGR5 (Kd: 0.86 nM) monoclonal antibody (mAb). Petosemtamab leads to blockade of EGFR signaling and receptor degradation in LGR5+ cancer cells. Petosemtamab can be used in the study of solid tumors such as head and neck squamous cell carcinoma (HNSCC), metastatic colorectal cancer (CRC), etc .
    Petosemtamab (FUT8-KO)
  • 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-P9977A
    Amivantamab (FUT8-KO)

    		EGFR Cancer
    Amivantamab (FUT8-KO) is a human EGFR-MET bispecific antibody with immune anticancer activity. Amivantamab (FUT8-KO) inhibits ligand binding, promotes endocytosis and degradation of receptor-antibody complexes, and induces Fc-dependent cytokinesis in macrophages and antibody-dependent cytotoxicity in natural killer cells .
    Amivantamab (FUT8-KO)
  • HY-164399
    SST0116CL1

    		HSP EGFR CDK Akt Cancer
    SST0116CL1 is a HSP90 inhibitor (IC50: 0.21 μM). SST0116CL1 binds to the ATP binding pocket of Hsp90, and interferes with Hsp90 chaperone function thus resulting in client protein (EGFR, CDK4 and AKT) degradation. SST0116CL1 induces degradation of Her2 in BT-474 cell (IC50: 0.2 μM). SST0116CL1 has antiproliferative activity and inhibits tumor growth .
    SST0116CL1
  • HY-163679
    PROTAC ERα Degrader-9

    		Estrogen Receptor/ERR Cytochrome P450 PROTACs Apoptosis Cancer
    PROTAC ERα Degrader-9 (Compound 18c) is a dual-targeting PROTAC degrader, which degrades estrogen receptor α (ERα) and aromatase (ARO). PROTAC ERα Degrader-9 binds to ERα with a Ki of 0.25 μM, inhibits ARO with an IC50 of 4.6 μM. PROTAC ERα Degrader-9 inhibits the proliferation of MCF-7 wildtype (IC50=0.54 μM) and ERα mutants MCF-7 EGFR (IC50=0.075 μM), MCF-7 D538G (IC50=0.31 μM), MCF-7 Y537S (IC50=2.3 μM), downregulates the expressions of ERS1 and MYC. PROTAC ERα Degrader-9 arrests the cell cycle at G2/M, induces apoptosis in MCF-7. PROTAC ERα Degrader-9 exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein (HY-163680); Black: linker (HY-W007559); Blue: ligand for E3 ligase (HY-112078))
    PROTAC ERα Degrader-9
  • HY-147219
    SIAIS164018

    		PROTACs Anaplastic lymphoma kinase (ALK) EGFR Apoptosis Cancer
    SIAIS164018 is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 exhibits better property than Brigatinib (HY-12857) .
    SIAIS164018
  • HY-147219A
    SIAIS164018 hydrochloride

    		PROTACs Anaplastic lymphoma kinase (ALK) EGFR Apoptosis Cancer
    SIAIS164018 hydrochloride is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 hydrochloride strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 hydrochloride exhibits better property than Brigatinib (HY-12857) .
    SIAIS164018 hydrochloride
  • HY-146325
    HSP90-IN-11

    		HSP Cancer
    HSP90-IN-11 (Compound 12c) is a potent inhibitor of HSP90. HSP90-IN-11 displays potent HSP90α inhibition comparable to AUY-922 (Luminespib). HSP90-IN-11 shows significant antiproliferative activity in CRC and NSCLC cells in a double digit nM range. HSP90-IN-11 leads to rapid degradation of client proteins EGFR and Akt in NSCLC cells. HSP90-IN-11 induces significant accumulation of a sub-G1 phase population .
    HSP90-IN-11

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