EGFR Degrader

EGFR Degraders (33):

Cat. No.	Product Name	Effect	Purity

HY-P99406

Petosemtamab	Degrader	99.94%
Petosemtamab (MCLA 158) is an anti- EGFR (K_d: 0.22 nM) and anti-LGR5 (K_d: 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).

HY-171265

Becotatug vedotin	Degrader
Becotatug vedotin (MRG003) is an Antibody-Drug Conjugate (ADC) that consists of an anti-EGFR humanized IgG1 monoclonal antibody Becotatug (HY-P990049) and MMAE (HY-15162). These two parts are connected through a valine-citrulline (valine-citrulline) linker, where the linker and MMAE constitute the ADC's Drug-Linker conjugate VcMMAE (HY-15575).

HY-156698

HJM-561	Degrader	99.26%
HJM-561 is a selective and effective orally active EGFR PROTAC degrader. HJM-561 is able to overcome the triple EGFR mutations that are resistant to Osimertinib (HY-15772). HJM-561 exhibits potent degradation of EGFR Del19/T790M/C797S (DC₅₀: 9.2 nM) and L858R/T790M/C797S (DC₅₀: 5.8 nM), and has anti-tumor activity (pink: EGFR ligand (HY-12857); blue: CRBN ligand (HY-A0003); black: linker).

HY-131864

SJF-1528	Degrader	98.90%
SJF-1528 (PROTAC 1) 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 mutant EGFR in HeLa cells. SJF-1528 also degrades HER2. SJF-1528 promotes ubiquitination and degradation of EGFR and can be used in breast cancer research (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-141676

HyT36	Degrader
HyT36 is a low molecular weight hydrophobic tag that promotes the degradation of fusion protein and pseudokinase Her3.

HY-131865

SJF-1521	Degrader	99.65%
SJF-1521 is a selective EGFR PROTAC degrader. SJF-1521 is capable of inducing EGFR degradation in OVCAR8 cells. SJF-1521 can be used for tumor research. (Pink: EGFR ligand (HY-177379); Black: Linker (HY-128804); Blue: VHL Ligand (HY-125845)).

HY-157581

MS39	Degrader	99.89%
MS39 (compound 6) is a PROTAC targeting EGFR. MS39 reduces the expression of EGFR and downstream signaling in HCC-827 and H3255 cells. MS39 inhibits the proliferation of H3255 cells.

HY-147941A

MS9427 TFA	Degrader	98.38%
MS9427 TFA is a potent PROTAC EGFR degrader with K_ds 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.

HY-153796

PROTAC Her3 Degrader-8	Degrader	99.60%
PROTAC Her3 Degrader-8 (Compound PP2) is a Her3 PROTAC degrader. PROTAC Her3 Degrader-8 promotes the ubiquitination and degradation of Her3. PROTAC Her3 Degrader-8 can be used in the study of lung adenocarcinoma and ovarian cancer (Pink: Her3 ligand (HY-107450); Blue: E3 ligase ligand (HY-170861); Black: linker (HY-Y1760)).

HY-161633

PROTAC EGFR degrader 11	Degrader	99.20%
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 K_i 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.

HY-175839

PROTAC EGFR degrader 15	Degrader	99.23%
PROTAC EGFR degrader 15 is a Pomalidomide (HY-10984)-based Gefitinib (HY-50895) EGFR PROTAC degrader. PROTAC EGFR degrader 15 triggers EGFR degradation via ubiquitin-proteasome-dependent proteolysis and autophagy-lysosome activation pathways. PROTAC EGFR degrader 15 targets ETFA to enhance ATP production. PROTAC EGFR degrader 15 significantly suppresses tumor growth in a Gefitinib-acquired resistant HCC-827 xenograft model. PROTAC EGFR degrader 15 can be used for the study of non-small cell lung cancer (NSCLC) (Pink: EGFR ligand (HY-W109039); Blue: CRBN ligand (HY-10984); Black: Linker (HY-W679737)).

HY-175252

PROTAC EGFR degrader 14	Degrader	99.26%
PROTAC EGFR degrader 14 is a potent and selective EGFR PROTACdegrader with a DC₅₀ of about 2.9 nM and a D_max of 93.1% for EGFR^{L858R/T790M/C797S}. PROTAC EGFR degrader 14 selectively induces EGFR^C797S degradation through a VHL and proteasome-dependent manner and downregulated EGFR-associated transcriptome and exhibits good selectivity over EGFR^WT. PROTAC EGFR degrader 14 induces cell cycle arrest and apoptosis and significantly inhibits tumor growth. PROTAC EGFR degrader 14 can be used for the study of nonsmall cell lung cancer (NSCLC) (Pink: Target protein ligand: (HY-143337); Blue: E3 ligand (HY-125845); Black: Linker (HY-W004688)).

HY-P99406A

Petosemtamab (FUT8-KO)	Degrader	99%
Petosemtamab (FUT8-KO) is an anti-EGFR and anti-LGR5 monoclonal antibody expressed in CHO cells with the fucosyltransferase 8 gene (FUT8) knocked out. Fucosyl loss enhances the ADCC effect of the antibody. Petosemtamab (FUT8-KO) leads to EGFR signaling blockade and receptor degradation in LGR5+ cancer cells. Petosemtamab (FUT8-KO) can be used for research on solid tumors such as head and neck squamous cell carcinoma (HNSCC) and metastatic colorectal cancer (CRC).

HY-131864A

SJF-1528 hemihydrate	Degrader	98.90%
SJF-1528 (PROTAC 1) hemihydrate 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 mutant EGFR in HeLa cells. SJF-1528 hemihydrate also degrades HER2. SJF-1528 hemihydrate promotes ubiquitination and degradation of EGFR and can be used in breast cancer research (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-177008

PROTAC HER2 degrader-1	Degrader	98.0%
PROTAC HER2 degrader-1 is a highly selective HER2 PROTAC degrader, with a DC₅₀ of 69 nM and a D_max of 96%. PROTAC HER2 degrader-1 inhibits HER2-positive cell proliferation and tumor growth through persistent HER2 degradation and potent inhibition of downstream pathways (AKT and ERK). PROTAC HER2 degrader-1 induces apoptosis in BT-474 cells. PROTAC HER2 degrader-1 can be used for research of HER2-positive cancers. (Pink: HER2 ligand: (HY-177009); Black: Linker; Blue: CRBN ligand: (HY-W023573).

HY-147941

MS9427	Degrader
MS9427 is a potent PROTAC EGFR degrader with K_ds 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.

HY-139997

DDC-01-163	Degrader	99.05%
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.

HY-172091

CZY43	Degrader
CZY43 is a HER3 degrader. CZY43 can effectively induce HER3 degradation in a dose- and time-dependent manner in breast cancer SKBR3 cells. CZY43 potently inhibits HER3-dependent signaling and cancer cell growth and outperforms Bosutinib (HY-10158).

HY-P991234

COVA208	Degrader
COVA208 is a bispecific FynomAb (a fusion protein of an antibody and a Fyn SH3-derived binding protein) that targets HER2. COVA208 induces the degradation of HER2, reduces the levels of HER2, HER3, and EGFR, thereby effectively blocking the downstream signaling pathways of HER2, including the HER3-PI3K-AKT and MAPK pathways, and simultaneously inducing apoptosis of tumor cells. COVA208 is promising for research of cancers, such as HER2-positive breast cancer, gastric cancer, and colorectal cancer.

HY-174415

ZSH-2117	Degrader
ZSH-2117 is a covalent and selective EGFR PROTAC degrader with a DC₅₀ of 45 nM in Ba/F3-EGFR^{L858R/T790M/C797S} cells. ZSH-2117 significantly inhibits cell proliferation and reduces the downstream EGFR signaling proteins level of AKT and ERK. ZSH-2117 effectively inhibits tumor growth in Ba/F3-EGFR^{L858R/T790M/C797S} xenograft mice model. Pink: EGFR ligand (HY-175162); Blue: NEDD4 ligase ligand (HY-175159); Black: linker

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