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EGFR ligand

" in MedChemExpress (MCE) Product Catalog:

By Targets:	E3 Ligase Ligand-Linker Conjugates (2) EGFR (15) Target Protein Ligand-Linker Conjugates (1) Apoptosis (3) Cytochrome P450 (1) DNA/RNA Synthesis (1) Estrogen Receptor/ERR (1) Ligands for Target Protein for PROTAC (3) PARP (2) PROTACs (9) VEGFR (1)
By Research Areas:	Cancer (20) Metabolic Disease (1)

Inhibitors & Agonists

Screening Libraries

Inhibitory Antibodies

Targets Recommended: EGFR Target Protein Ligand-Linker Conjugates E3 Ligase Ligand-Linker Conjugates PD-1/PD-L1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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) .

HY-141640

MS154	PROTACs EGFR	Cancer
MS154 is a first-in-class E3 ligase cereblon-recruiting *EGFR* degrader with K_ds of 1.8 nM and 3.8 nM for EGFR ^WT and EGFR ^L858R mutants. MS154 potently induces the degradation of mutant but not wild-type EGFR in an E3 ligase-dependent manner in cancer cell lines. MS154 potently inhibits cell proliferation in lung cancer cells (Blue: E3 Ligase ligand (HY-103596); Black: linker (HY-W096167); Pink: EGFR ligand (HY-168305)) .

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 K_d 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)) .

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)) .

HY-150905

EGFR ligand-2	EGFR	Cancer
EGFR ligand-2 (compound C4), a covalent *EGFR* ligand, is a EGFR mutant inhibitor with IC₅₀s of 21 nM and 48 nM for EGFR ^L858R and EGFR ^L858R/T790M, respectively. EGFR ligand-2 can be used to synthesize PROTAC .

HY-168305

EGFR ligand-11	Ligands for Target Protein for PROTAC EGFR	Cancer
EGFR ligand-11 is a target protein ligand for *EGFR* and can be used to synthesize PROTAC MS154 (HY-141640) .

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 .

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 .

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)) .

HY-170350

Pomalidomide-PEG2-OMs	E3 Ligase Ligand-Linker Conjugates	Cancer
Pomalidomide-PEG2-Oms (CRBN ligand Pomalidomide (HY-10984)) is an E3 Ligase Ligand-Linker Conjugate for EGFR PROTAC DDC-01-163 (HY-139997) .

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))

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 .

HY-P9968

Nimotuzumab	EGFR	Cancer
Nimotuzumab is a humanized IgG1 monoclonal antibody targeting *EGFR* with a K_D of 0.21 nM. Nimotuzumab is directed against the extracellular domain of the EGFR blocking the binding to its ligands. Nimotuzumab, a strong antitumor agent, is cytolytic on target tumors by its capacity to cause antibody dependent cell mediated cytotoxicity (ADCC) and complement dependent cytotoxicity (CDC) .

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) .

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 .

HY-157581

MS39	PROTACs EGFR	Cancer
MS39 (compound 6) is a PROTAC targeting *EGFR. MS39 is composed of PROTAC target protein ligand* N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-(3-(piperazin-1-yl)propoxy)quinazolin-4-amine (HY-W109039) (red part), E3 ligase ligand (S,R,S)-AHPC (HY-125845) (blue part) and PROTAC Linker Undecanedioic acid (HY-W014125) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is (S,R,S)-AHPC-CO-C9-acid (HY-139345). MS39 reduces the expression of EGFR and downstream signaling in HCC-827 and H3255 cells. MS39 inhibits the proliferation of H3255 cells .

HY-157579

MS154N	PROTACs EGFR	Cancer
MS154N (compound 28) is the negative control of MS39 (HY-157581). MS154N is composed of PROTAC target protein ligand EGFR ligand-11 (HY-168305) (red part), E3 ligase ligand 4-Hydroxy-2-(1-methyl-2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione (HY-W441376) (blue part) and PROTAC Linker 8-Iodooctan-1-amine (HY-168306) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is Me-Thalidomide-O-C8-NH2 (HY-168307) .

HY-P9977A

Amivantamab (FUT8-KO)	EGFR	Cancer
Amivantamab (FUT8-KO) is an anti-EGFR-MET monoclonal antibody expressed by CHO cells with the fucosyltransferase 8 gene (FUT8) knocked out. Fucose deficiency enhances the ADCC effect of the antibody. 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 .

HY-116624

MAZ51 4 Publications Verification	VEGFR Apoptosis	Cancer
MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Antitumor activity .

HY-165060

(±)2-(14,15-Epoxyeicosatrienoyl) glycerol (±)2-14,15-EG	DNA/RNA Synthesis	Metabolic Disease
(±)2-(14,15-Epoxyeicosatrienoyl) glycerol ((±)2-14,15-EG) is a novel CYP450 metabolite of 2-Arachidonoyl glycerol (2-AG) in the kidney. (±)2-(14,15-Epoxyeicosatrienoyl) glycerol is a potent mitogen for renal epithelial cells, increasing DNA synthesis in LLCPKcl4 cells. (±)2-(14,15-Epoxyeicosatrienoyl) glycerol activates the metalloprotease ADAM17, which cleaves proTGF-α and releases TGF-α as a ligand that initiates the EGFR-ERK signalling pathway .

HY-75706

N-Descyclopropanecarbaldehyde Olaparib	PARP Ligands for Target Protein for PROTAC	Cancer
N-Descyclopropanecarbaldehyde Olaparib is an analogue of Olaparib (HY-10162) containing DOTA moiety. N-Descyclopropanecarbaldehyde Olaparib is a PARP inhibitor used for synthesizing novel dual EGFR and PARP PROTAC, DP-C-4 . N-Descyclopropanecarbaldehyde Olaparib can be radiolabeled F-18 or fluorophore for positron emission tomography (PET) or optical imaging in several types of tumor .

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 K_i 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))

Cat. No.	Product Name

HY-L016

Protein Tyrosine Kinase Compound Library	1,259 compounds
Protein tyrosine kinases (PTKs) are key signaling molecules and important drug targets. Two classes of PTKs are present in cells: the transmembrane receptor PTKs (RTKs) and the nonreceptor PTKs. The RTK family includes the receptors for insulin and for many growth factors, such as EGFR, FGFR, PDGFR, VEGFR, and NGFR. RTKs are transmembrane glycoproteins that are activated by the binding of their ligands, and they transduce the extracellular signal to the cytoplasm by phosphorylating tyrosine residues on the receptors themselves (autophosphorylation) and on downstream signaling proteins. Their principal functions of PTKs involve the regulation of multicellular aspects of the organism. Cell to cell signals concerning growth, differentiation, adhesion, motility, and death are frequently transmitted through tyrosine kinases. In humans, tyrosine kinases have been demonstrated to play significant roles in the development of many disease states, including diabetes and cancers. MCE designs a unique collection of 1,259 compounds that act as a useful tool for PTKs-related drug screening and disease research.

Protein Tyrosine Kinase Compound Library

1,259 compounds

Protein tyrosine kinases (PTKs) are key signaling molecules and important drug targets. Two classes of PTKs are present in cells: the transmembrane receptor PTKs (RTKs) and the nonreceptor PTKs. The RTK family includes the receptors for insulin and for many growth factors, such as EGFR, FGFR, PDGFR, VEGFR, and NGFR. RTKs are transmembrane glycoproteins that are activated by the binding of their ligands, and they transduce the extracellular signal to the cytoplasm by phosphorylating tyrosine residues on the receptors themselves (autophosphorylation) and on downstream signaling proteins. Their principal functions of PTKs involve the regulation of multicellular aspects of the organism. Cell to cell signals concerning growth, differentiation, adhesion, motility, and death are frequently transmitted through tyrosine kinases. In humans, tyrosine kinases have been demonstrated to play significant roles in the development of many disease states, including diabetes and cancers.

MCE designs a unique collection of 1,259 compounds that act as a useful tool for PTKs-related drug screening and disease research.

Cat. No.	Product Name	Target	Research Area

HY-P9968

Nimotuzumab	EGFR	Cancer
Nimotuzumab is a humanized IgG1 monoclonal antibody targeting *EGFR* with a K_D of 0.21 nM. Nimotuzumab is directed against the extracellular domain of the EGFR blocking the binding to its ligands. Nimotuzumab, a strong antitumor agent, is cytolytic on target tumors by its capacity to cause antibody dependent cell mediated cytotoxicity (ADCC) and complement dependent cytotoxicity (CDC) .

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 .

HY-P9977A

Amivantamab (FUT8-KO)	EGFR	Cancer
Amivantamab (FUT8-KO) is an anti-EGFR-MET monoclonal antibody expressed by CHO cells with the fucosyltransferase 8 gene (FUT8) knocked out. Fucose deficiency enhances the ADCC effect of the antibody. 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 .

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