EGFR/HER2

Cat. No.

A23972

MS9427 TFA

MS9427 TFA is a potent PROTAC degrader targeting EGFR, with binding affinities (K_d) of 7.1 nM for wild-type EGFR and 4.3 nM for the EGFR L858R mutant. It selectively degrades the mutant EGFR via both the ubiquitin–proteasome system (UPS) and autophagy–lysosome pathways. MS9427 TFA effectively inhibits the proliferation of non-small cell lung cancer (NSCLC) cells and is a valuable tool for anticancer research focused on EGFR-driven malignancies.

Cat. No.

A23980

SIAIS164018 hydrochloride

SIAIS164018 hydrochloride is a PROTAC-based dual degrader targeting ALK and EGFR, with IC₅₀ values of 2.5 nM for ALK and 6.6 nM for the ALK G1202R mutant. It effectively suppresses cancer cell migration and invasion, induces G1 phase cell cycle arrest, and promotes apoptosis, making it a promising candidate for targeted cancer therapy research.

Cat. No.

A24002

CAS No.

2230821-40-4

SJF-1521

SJF-1521 is a selective PROTAC degrader targeting the epidermal growth factor receptor (EGFR). It incorporates lapatinib, a known EGFR inhibitor, as the targeting ligand and promotes proteasomal degradation of EGFR. SJF-1521 effectively induces EGFR degradation in OVCAR8 ovarian cancer cells, offering a promising strategy for disrupting EGFR signaling in EGFR-driven malignancies.

Cat. No.

A24093

CAS No.

2772612-96-9

MS9449

MS9449 is a potent PROTAC-based degrader of the epidermal growth factor receptor (EGFR), exhibiting strong binding affinities with K\_d values of 17 nM for wild-type EGFR and 10 nM for the L858R mutant. It effectively induces degradation of mutant EGFR proteins via both the ubiquitin–proteasome system (UPS) and the autophagy–lysosome pathway, enabling dual-pathway clearance. MS9449 shows strong antiproliferative activity in non-small cell lung cancer (NSCLC) cells, making it a valuable compound for anticancer research, particularly in EGFR-driven tumors.

Cat. No.

A24099

CAS No.

2675490-92-1

MS39

MS-39 is a highly potent and selective PROTAC degrader specifically engineered to target mutant forms of the epidermal growth factor receptor (EGFR). It is constructed by conjugating the EGFR inhibitor gefitinib to a von Hippel–Lindau (VHL) E3 ligase ligand via a tailored linker. MS-39 exhibits strong binding affinity and efficient degradation of mutant EGFR proteins, offering a promising strategy for overcoming resistance in EGFR-driven cancers. Its design enables targeted proteasomal degradation rather than mere kinase inhibition, providing a novel approach to cancer therapy.

Cat. No.

A24846

CAS No.

2550393-21-8

MS154

MS154 is a novel E3 ligase cereblon-recruited degrader specifically targeting epidermal growth factor receptor (EGFR). It has demonstrated potent degradation of the EGFR L858R mutant in cancer cell lines with Kd values of 1.8 nM and 3.8 nM for wild-type and mutant EGFR, respectively. This selective degradation mechanism highlights its potential as an anticancer agent, particularly in lung cancer treatment. MS154 operates through an E3 ligase-dependent pathway, representing a promising therapeutic strategy for treating EGFR-driven malignancies.

Cat. No.

A28640

CAS No.

2768472-28-0

PROTAC EGFR degrader 3

PROTAC EGFR Degrader 3 is a potent PROTAC designed to selectively target and degrade mutant EGFR proteins. It demonstrates remarkable cellular activity in H1975 and HCC827 cell lines, effectively facilitating the lysosomal degradation of EGFR mutants. This compound is particularly useful for research applications focused on targeted protein degradation and the study of EGFR-related signaling pathways in cancer.

Cat. No.

A28760

CAS No.

2861227-35-0

PROTAC EGFR degrader 13

PROTAC EGFR Degrader 13 is a targeted protein degradation compound that selectively degrades the epidermal growth factor receptor (EGFR). This degrader exhibits potent antiproliferative activity with an IC50 of 15.6 nM against Ba/F3 cells harboring the EGFR T790M-L858R-C797S mutations, demonstrating its effectiveness in EGFR-related cancer research. This reagent is suitable for investigating the underlying mechanisms of EGFR-driven malignancies and developing therapeutic strategies focused on targeted degradation pathways.

Cat. No.

A28813

CAS No.

2140806-84-2

DDC-01-163

DDC-01-163 is an allosteric PROTAC degrader that targets the epidermal growth factor receptor (EGFR) through the ubiquitin-proteasome system. It demonstrates selective inhibition of L858R/T790M mutant Ba/F3 cell proliferation and is effective against resistant variants, including L/T/C797S and L/T/L718Q EGFR mutations. DDC-01-163 exhibits enhanced anti-proliferative effects in combination with the ATP-site EGFR inhibitor Osimertinib, making it a valuable tool for studying non-small cell lung cancer.

Cat. No.

A28875

CAS No.

2772613-37-1

MS9427

MS9427 is a selective PROTAC degrader targeting the epidermal growth factor receptor (EGFR), demonstrating Kd values of 7.1 nM and 4.3 nM for EGFR wild-type and L858R mutant forms, respectively. This compound effectively induces degradation of the mutant EGFR via both the ubiquitin/proteasome system and autophagy/lysosomal pathways, while sparing the wild-type receptor. MS9427 is a valuable tool for studying the proliferation inhibition of non-small cell lung cancer (NSCLC) cells and advancing anticancer research.

Cat. No.

A28886

CAS No.

2675490-97-6

MS154N

MS154N is a negative control for the selective degradation of target proteins via the PROTAC (proteolysis targeting chimera) approach. Comprising an EGFR ligand, an E3 ligase ligand, and a PROTAC linker, this compound serves as a crucial investigational tool for validating the specificity and efficacy of PROTAC-based assays. Its design facilitates research into targeted protein degradation mechanisms, providing a reliable reference for experimental protocols involving MS39.

Cat. No.

A28937

CAS No.

2925923-46-0

PROTAC EGFR degrader 8

PROTAC EGFR Degrader 8 (T-184) is a proteolysis-targeting chimera (PROTAC) that specifically degrades the epidermal growth factor receptor (EGFR). With a DC50 of 15.56 nM in HCC827 cells, it effectively reduces EGFR levels and demonstrates potent growth inhibition in H1975, PC-9, and HCC827 cell lines, exhibiting IC50 values of 7.72 nM, 121.9 nM, and 14.21 nM, respectively. This compound is valuable for research focusing on cancer biology, particularly non-small cell lung cancer (NSCLC).

Cat. No.

A28941

CAS No.

3031336-58-7

PROTAC EGFR degrader 2

PROTAC EGFR Degrader 2 is a highly effective small molecule that targets the epidermal growth factor receptor (EGFR) for degradation via the PROTAC mechanism. It demonstrates significant antiproliferative activity with an IC50 of 4.0 nM, along with robust EGFR degradation activity, exhibiting a DC50 of 36.51 nM. This compound is suitable for applications in cancer research, particularly in exploring EGFR-related pathways and developing nitroreductase (NTR)-responsive PROTAC systems.

Cat. No.

A28945

CAS No.

2882845-50-1

PROTAC EGFR degrader 4

PROTAC EGFR Degrader 4 is a highly selective PROTAC designed to target mutant epidermal growth factor receptor (EGFR) variants. It effectively induces the degradation of EGFR del19 and the EGFR L858R/T790M double mutant, with DC50 values of 0.51 nM and 126 nM, respectively. This compound demonstrates significant growth inhibition in HCC827 and H1975 cell lines, exhibiting IC50 values of 0.83 nM and 203.1 nM. The degradation of EGFR is associated with autophagy, highlighting its potential in cancer research and therapeutic applications.

Cat. No.

A84556

CAS No.

2661609-36-3

DP-C-4

DP-C-4 is a Cereblon-based dual-targeting PROTAC molecule designed for the concurrent degradation of epidermal growth factor receptor (EGFR) and poly (ADP-ribose) polymerase (PARP). This compound demonstrates significant biological activity by promoting the targeted destruction of these proteins, which can be crucial in cancer research and therapeutic applications. DP-C-4 may facilitate studies investigating the interplay between EGFR and PARP pathways, potentially leading to new insights in oncology and the development of innovative treatment strategies.