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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
64 Results for "
PROTAC EGFR
" in MedChemExpress (MCE) Product Catalog:
Products (64)
64 Results for "PROTAC EGFR" in MCE Product Catalog:
4
4 Cited Publications
Gefitinib-based PROTAC 3 is a PROTAC degrader targeting EGFR, with a DC50 of 11.7 nM against exon 19 deletion mutants and a DC50 of 22.3 nM against EGFR L858R. Gefitinib-based PROTAC 3 selectively induces the ubiquitin-proteasome degradation of exon 19 deletion-mutant and L858R-mutant EGFR by recruiting the VHL E3 ligase. Gefitinib-based PROTAC 3 can be used for the research of EGFR mutation-positive cancers .
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) .
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QCA570 is a pan-BET-BRD PROTAC degrader. QCA570 degrades BRD2/3/4 and BRDT via cereblon and the ubiquitin-proteasome pathway, inhibits the expression of c-MYC, EZH2 and Mcl-1, induces tumor cell apoptosis, cycle arrest and regression, and exerts a synergistic inhibitory effect on Osimertinib (HY-15772)-resistant EGFR-mutant non-small cell lung cancer. QCA570 can be used in the research of acute myeloid leukemia, acute lymphoblastic leukemia, bladder cancer and non-small cell lung 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.
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 .
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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 .
PROTAC EGFR degrader 4 is an EGFR del19 and EGFR L858R/T790M degrader with anti-proliferative activity. PROTAC EGFR degrader 4 induces degradation of mutant EGFR variants via ubiquitination and autophagy. PROTAC EGFR degrader 4 suppresses EGFR pathway signal transduction. PROTAC EGFR degrader 4 induces apoptosis, arrests cell cycle, and suppresses cell colony formation in cancer cells. PROTAC EGFR degrader 4 can be used for the research of non-small cell lung cancer .
Cat. No.: HY-175839
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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) .
Cat. No.: HY-161536
CAS No.: 2992670-33-2
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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)) .
Cat. No.: HY-75706
CAS No.: 763111-47-3
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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 (HY-141481) . N-Descyclopropanecarbaldehyde Olaparib can be radiolabeled with F-18 or fluorophore for positron emission tomography (PET) or optical imaging in several types of tumor .
PROTAC EGFR degrader 2 is an EGFR-targeting PROTAC and antitumor agent. PROTAC EGFR degrader 2 induces degradation of EGFR protein via the ubiquitin-proteasome system, requiring binding to both EGFR and the VHL E3 ubiquitin ligase. PROTAC EGFR degrader 2 exerts antitumor efficacy following EGFR degradation. PROTAC EGFR degrader 2 is released from the NTR-responsive caged-PROTAC 17-1 upon activation by nitroreductase in hypoxic tumor tissues. PROTAC EGFR degrader 2 can be used for the research of non-small cell lung cancer .
Cat. No.: HY-175252
PROTAC EGFR degrader 14 is a EGFR PROTAC degrader, with a DC50 of 2.9 nM against EGFR L858R/T790M/C797S. PROTAC EGFR degrader 14 forms a stable ternary complex by bridging the ATP-binding pocket of the target protein EGFR with VHL E3 ubiquitin ligase, induces efficient and specific degradation of EGFR mutants via the ubiquitin-proteasome system, and ultimately induces cell cycle arrest and apoptosis. PROTAC EGFR degrader 14 can be used in studies related to non-small cell lung cancer carrying the EGFR C797S drug-resistant mutation .
Cat. No.: HY-161633
CAS No.: 3034244-71-5
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.
Cat. No.: HY-139997
CAS No.: 2140806-84-2
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 .
PROTAC EGFR degrader 8 (T-184) is a PROTAC degrader that targets EGFR for degradation by recruiting cereblon. It induces EGFR protein degradation with a DC50 of 10.18 nM. The IC50 values of PROTAC EGFR degrader 8 for inhibiting the growth of H1975, PC-9 and HCC827 cells are 7.72, 121.9 and 14.21 nM, respectively. PROTAC EGFR degrader 8 inhibits the proliferation of EGFR-mutant non-small cell lung cancer cells and can be used in studies related to non-small cell lung cancer .
Cat. No.: HY-161537
CAS No.: 2992670-44-5
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EGFR ligand-9 is an EGFR ligand. EGFR ligand-9 can be used for synthesis of PROTAC EGFR degrader 9 (HY-161536) .
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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 .
MS9449 is a potent PROTAC EGFR degrader, with Kd values of 17 nM and 10 nM for wild-type EGFR and mutant EGFR L858R, respectively, and a DC50 of 7.1 nM for EGFR Del19. MS9449 effectively induces the degradation of mutant EGFR through the ubiquitin-proteasome system (UPS) and the autophagy-lysosome pathway. MS9449 exhibits anticancer activity against non-small cell lung cancer. MS9449 can be applied in related research on non-small cell lung cancer .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
