Search Result
Results for "
PROTAC EGFR
" in MedChemExpress (MCE) Product Catalog:
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-123921
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PROTACs
EGFR
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Cancer
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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 .
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- HY-156698
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PROTACs
EGFR
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Cancer
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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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- HY-147858
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PROTACs
EGFR
Apoptosis
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Cancer
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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.
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- HY-141640
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PROTACs
EGFR
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Cancer
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MS154 is a first-in-class E3 ligase cereblon-recruited EGFR degrader with Kd values of 1.8 nM and 3.8 nM for EGFR WT and EGFR L858R mutant, respectively. MS154 potently induces degradation of mutant, but not wild-type, EGFR in cancer cell lines in an E3 ligase-dependent manner. MS154 exhibits anticancer effects against lung cancer (blue: E3 ligase ligand (HY-103596); black: linker (HY-W096167); pink: EGFR ligand (HY-168305)) .
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- HY-131864
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PROTACs
EGFR
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Cancer
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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)) .
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- HY-130549
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PROTAC Linkers
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Cancer
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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 .
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- HY-146349
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PROTACs
EGFR
Autophagy
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Cancer
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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 .
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- HY-161536
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PROTACs
EGFR
Apoptosis
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Cancer
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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)) .
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- HY-175839
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PROTACs
EGFR
ATP Synthase
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Cancer
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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) (Pink: EGFR ligand (HY-W109039); Blue: CRBN ligand (HY-10984); Black: Linker (HY-W679737)) .
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- HY-75706
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PARP
Ligands for Target Protein for PROTAC
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Cancer
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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 .
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- HY-157581
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EGFR
PROTACs
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Cancer
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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 .
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- HY-131865
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PROTACs
EGFR
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Cancer
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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)) .
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- HY-175252
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PROTACs
EGFR
Apoptosis
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Cancer
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PROTAC EGFR degrader 14 is a potent and selective EGFR PROTACdegrader with a DC50 of about 2.9 nM and a Dmax 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)) .
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- HY-144304
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PROTACs
EGFR
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Cancer
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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 .
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- HY-139997
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PROTACs
EGFR
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Cancer
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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 .
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- HY-161633
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PROTACs
EGFR
FAK
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Cancer
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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.
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- HY-153901
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EGFR
PROTACs
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Cancer
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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 .
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- HY-178861
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PROTACs
CDK
Caspase
PARP
Apoptosis
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Cancer
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dCDK9-202 a potent CDK9 PROTAC degrader with an DC50 value of 3.5 nM. dCDK9-202 exhibits broad-spectrum anti-tumor activity and extensively disrupts the oncogenic transcriptome. dCDK9-202 can activate Caspase-3/7, increase the level of cleaved PARP, and directly induce apoptosis of tumor cells. dCDK9-202 effectively inhibits TC-71 tumor growth without any signs of toxicity in mice. dCDK9-202 can be used for the study of EGFR-driven cancers such as sarcoma (Pink: CDK9 ligand (HY-178862); Blue: CRBN ligand (HY-W248665); Black: Linker (HY-N8015)) .
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- HY-161537
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EGFR
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Cancer
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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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- HY-147942
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PROTACs
EGFR
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Cancer
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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 .
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- HY-147941
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PROTACs
EGFR
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Inflammation/Immunology
Cancer
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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 .
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- HY-157579
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PROTACs
EGFR
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Cancer
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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) .
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- HY-178242
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PROTACs
EGFR
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Cancer
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PROTAC EGFR degrader 16 (Compound 98) a selective EGFR PROTAC degrader with DC50 values of < 50 nM in NCI-H1975 (EGFR L858R-T970M), NCI-H3225 (EGFR L858R) and NCI-H1976 + CS (EGFR L858R-T970M-L797S). PROTAC EGFR degrader 16 can be used for the study of EGFR-driven cancerssuch as non-small cell lung cancer (Pink: EGFR ligand (HY-178313); Blue: CRBN ligand (HY-W1128702); Black: Linker; EGFR ligand + Linker (HY-178311)) .
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- HY-147219A
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PROTACs
Anaplastic lymphoma kinase (ALK)
EGFR
Apoptosis
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Cancer
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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) .
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- HY-144605
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EGFR
PROTACs
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Cancer
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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 .
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- HY-171958
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PROTACs
EGFR
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Cancer
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PROTAC EGFR degrader 12 (example 1) is a PROTAC degrader targeting EGFR that can effectively degrade EGFR mutants, but has little effect on EGFR WT. PROTAC EGFR degrader 12 shows IC50s against EGFR L858R-T790M (NCI-H1975 cells), EGFR L858R (NCI-H3255 cells), and EGFR L858R-T790M-L797S (NCI-H1975+CS cells) of all <50 nM .
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- HY-141481
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PROTACs
EGFR
PARP
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Cancer
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DP-C-4 is a Cereblon-based dual PROTAC for simultaneous degradation of EGFR and PARP .
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- HY-147941A
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PROTACs
EGFR
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Infection
Inflammation/Immunology
Cancer
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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 .
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- HY-147219
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PROTACs
Anaplastic lymphoma kinase (ALK)
EGFR
Apoptosis
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Cancer
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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) .
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- HY-161632
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PROTACs
EGFR
FAK
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Cancer
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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 .
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- HY-146423
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PROTACs
EGFR
Apoptosis
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Cancer
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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 .
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- HY-146422
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PROTACs
EGFR
Apoptosis
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Cancer
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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 .
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- HY-158313
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EGFR
PROTACs
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Cancer
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PROTAC EGFR degrader 13 (compound 106) is an EGFR PROTAC degrader with a DC50 of <0.1 μM. PROTAC EGFR degrader 13 has proliferation inhibitory activity on cell Ba/F3-TEL-EGFR-T790M-L858R-C797S with an IC50 of 15.6 nM. PROTAC EGFR degrader 13 can be used for the study of EGFR-related diseases such as cancer (Pink: Target protein ligand; Blue: E3 ligand (HY-14658); Black: linker (HY-W262798); E3 ligand + linker: HY-W998306) .
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- HY-150905
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EGFR
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Cancer
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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 .
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- HY-178311
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- HY-178313
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Ligands for Target Protein for PROTAC
EGFR
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Cancer
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EGFR ligand-18 is a PROTAC target protein ligand that can be used for synthesis of PROTACs, such as PROTAC EGFR degrader 16 (HY-178242). PROTAC EGFR degrader 16 is a potent EGFR PROTAC degrader with anti-tumor activity .
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- HY-175887
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Pomalidomide-C9-Br is a synthesized E3 ligase ligand-linker conjugate that can be used to synthesize PROTAC EGFR degrader 15 (HY-175839). PROTAC EGFR degrader 15 is a potent EGFR PROTAC degrader with anti-cancer activity .
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- HY-176788
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Target Protein Ligand-Linker Conjugates
EGFR
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Cancer
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EGFR Ligand-Linker Conjugates 1 is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for EGFR (HY-150905) and a PROTAC linker, which recruits E3 ligases. EGFR Ligand-Linker Conjugates 1 can be used for synthesis of PROTAC EGFR degrader 3 (HY-144605) .
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- HY-156700
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PROTAC Linkers
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Cancer
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Lenalidomide-acetylene-Br is a PROTAC Linker taht makes up HJM-561 (HY-156698). HJM-561 is a potent, selective, and orally active EGFR PROTAC to inhiibit Osimertinib (HY-15772)-resistant EGFR triple mutations.
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- HY-W262798
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PMP
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PROTAC Linkers
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Cancer
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1-(Piperidin-4-ylmethyl)piperazine is a PROTAC linker. 1-(Piperidin-4-ylmethyl)piperazine can be used to design PROTAC, such as PROTAC EGFR degrader 13 (HY-158313) .
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- HY-131864A
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PROTACs
EGFR
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Cancer
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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)) .
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- HY-174415
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PROTACs
EGFR
Akt
ERK
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Cancer
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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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- HY-141486A
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- HY-141486
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Target Protein Ligand-Linker Conjugates
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Cancer
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(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 .
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- HY-147858A
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PROTACs
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Cancer
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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 .
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- HY-175255
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Target Protein Ligand-Linker Conjugates
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Cancer
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EGFR-IN-47-C6-COOMe is a synthesized target protein ligand-linker conjugate that can be used for synthesis of PROTACs, such as PROTAC EGFR degrader 14 (HY-175252). PROTAC EGFR degrader 14 is a EGFR PROTAC degrader with anti-tumor activity .
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- HY-161538
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- HY-168305
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- HY-161613
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- HY-170350
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- HY-180917
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PROTACs
EGFR
Ligands for E3 Ligase
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Cancer
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PROTAC EGFR degrader 17 (Compound 35) is an EGFR PROTAC degrader with a DC50 value of 0.49 nM. PROTAC EGFR degrader 17 promotes the ubiquitination and degradation of EGFR. PROTAC EGFR degrader 17 can be used in research on various cancers, including non-small cell lung cancer .
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- HY-163679
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Estrogen Receptor/ERR
Cytochrome P450
PROTACs
Apoptosis
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Cancer
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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))
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- HY-181115
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- HY-W109039
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- HY-W998306
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Pomalidomide 5'-piperazine-4-methylpiperidine is the conjugate composed of a E3 ligase ligand and a linker. Pomalidomide 5'-piperazine-4-methylpiperidine can be used for PROTAC synthesis, such as PROTAC EGFR degrader 13 (HY-158313) .
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- HY-175948
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E3 Ligase Ligand-Linker Conjugates
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Others
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Lenalidomide-CO-C3-NH-alkynes is an E3 ligase ligand-linker conjugate comprising Lenalidomide (HY-A0003) and a linker. Acepromazine-1-piperazinepropanamine dihydrochloride can be conjugated to a target protein ligand to form a PROTAC molecule—for instance, the PROTAC EGFR degrader 7 (HY-147858) .
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- HY-180964
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PROTACs
Anaplastic lymphoma kinase (ALK)
EGFR
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Cancer
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Lys-PEG3-BA is an EML4-ALK/EGFR PROTAC degrader with DC50 values of 1.32 and 19.66 μM for H3122 (EML4-ALK) and H1975 (EGFR-L858R/T790M) cells, respectively. Lys-PEG3-BA hinders proliferation via rewiring the ubiquitin- proteasome system in vitro. Lys-PEG3-BA can be used for non-small cell lung cancer research .
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- HY-180965
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PROTACs
Anaplastic lymphoma kinase (ALK)
EGFR
Apoptosis
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Cancer
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Pro-PEG3-BA is an EML4-ALK/EGFR PROTAC degrader, degrading EML4 ALK and EGFR mutant (L858R/T790M) with DC 50 values of 0.42 and 13.50 μM, respectively. Pro-PEG3-BA hinders proliferation and induces cell cycle arrest and apoptosis of NSCLC cells in vitro. Pro-PEG3-BA shows safety profile and decreases EML4-ALK protein via rewiring the ubiquitin- proteasome system in vivo. Pro-PEG3-BA can be used for non-small cell lung cancer research .
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- HY-180966
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PROTACs
EGFR
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Cancer
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Gly-PEG3-BA is an EML4-ALK PROTAC degrader. Gly-PEG3-BA effectively reduces EML4-ALK with a DC50 value of 0.50 μM in H3122 (EML4-ALK) cells. Gly-PEG3-BA effectively reduces EGFR mutant (L858R/T790M) levels with a DC50 of 20.15 μM in H1975 (EGER-L858R/T790M) cells. Gly-PEG3-BA exerts potent antiproliferation activity in H3122 (EML4-ALK) and H1975 (EGER-L858R/T790M) cells with IC50s value of 0.84 and 20.74 μM. Gly-PEG3-BA can be used for non-small lung cancer research .
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Classification |
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- HY-147858
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Alkynes
PROTAC Synthesis
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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.
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- HY-175948
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Alkynes
PROTAC Synthesis
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Lenalidomide-CO-C3-NH-alkynes is an E3 ligase ligand-linker conjugate comprising Lenalidomide (HY-A0003) and a linker. Acepromazine-1-piperazinepropanamine dihydrochloride can be conjugated to a target protein ligand to form a PROTAC molecule—for instance, the PROTAC EGFR degrader 7 (HY-147858) .
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