EGFR Degrader

PROTAC EGFR degrader 1 (Racemate of compound 1002) is a VHL-recruiting EGFR PROTAC degrader. PROTAC EGFR degrader 1 brings EGFR into proximity with the VHL ubiquitin ligase, enabling ubiquitination and degradation of EGFR. PROTAC EGFR degrader 1 can be used in cancer research.

PROTAC EGFR degrader 6 is a PROTAC-based degrader and inducer targeting EGFRdel19. PROTAC EGFR degrader 6 induces the degradation of EGFRdel19 via the ubiquitin-proteasome system. PROTAC EGFR degrader 6 induces apoptosis. PROTAC EGFR degrader 6 arrests cells at the G1 phase. PROTAC EGFR degrader 6 can be used in research related to non-small cell lung cancer.

(Rac)-Zearalanone-d₆ is the d₆-labeled (Rac)-Zearalanone (HY-N6678A). (Rac)-Zearalanone is an ATP-competitive HSP90 inhibitor with an EC₅₀ of 2.3 μM. (Rac)-Zearalanone interferes with the binding of ATP to HSP90, impairs the chaperone function of HSP90, and promotes the degradation of client proteins. (Rac)-Zearalanone reduces intracellular accumulation of Raf-1, induces cleavage of caspase-3, and promotes Her2 degradation in a dose-dependent manner by disrupting the Her2-HSP90 interaction. (Rac)-Zearalanone can be used in the research of small cell lung cancer and breast cancer.

HDTAC EGFR Degrader-1 is an EGFR HDTAC (hypoxia-activated targeted protein degradation chimera) degrader with a DC₅₀ of 1.76 μM. HDTAC EGFR Degrader-1 consists of a linker, a tumor hypoxia-activated group (HAG, a group that generates ROS under tumor hypoxic conditions), and an EGFR ligand. HDTAC EGFR Degrader-1 drives EGFR degradation through the proteasomal pathway. HDTAC EGFR Degrader-1 downregulates Caspase-3 under hypoxic conditions. HDTAC EGFR Degrader-1 can be used in research on non-small cell lung cancer harboring EGFR mutations (EGFR ligand: FAAH-IN-2 (HY-79511); HAG: Thalidomide-O-COOH (HY-103597); linker: NH2-PEG3 (HY-W007545)).

PROTAC Her3 Degrader-2 is a Her3 PROTAC degrader with an IC₅₀ < 10 nM. PROTAC Her3 Degrader-2 recruits Her3 to E3 ubiquitin ligase to achieve selective degradation. PROTAC Her3 Degrader-2 can be used in the research of breast cancer, lung cancer, head and neck cancer, and prostate cancer.

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.

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.

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.

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 IC_{50s 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.}

SST0116CL1 is a HSP90 inhibitor (IC₅₀: 0.21 μM). SST0116CL1 binds to the ATP binding pocket of Hsp90, and interferes with Hsp90 chaperone function thus resulting in client protein (EGFR, CDK4 and AKT) degradation. SST0116CL1 induces degradation of Her2 in BT-474 cell (IC₅₀: 0.2 μM). SST0116CL1 has antiproliferative activity and inhibits tumor growth. SST0116CL1 can be used for the study of leukemia, gastric and ovarian carcinoma.

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.

Ctx-L3 is a selective EGFR PTAC (PSMA-targeted chimera) degrader (DC₅₀: 4.3 pM in LNCaP cells) and LYTAC. Ctx-L3 recruits prostate-specific membrane antigen (PSMA) and mediates lysosomal degradation of EGFR in PSMA-positive prostate cancer cells. Ctx-L3 exhibits degrading activity against EGFR in prostate cancer cells. Ctx-L3 is applicable to related research on prostate cancer.

EGFR ligand-10 is an EGFR ligand and can be used for the synthesis of PROTACs, such as SJF-1528 (HY-131864).

G3130 is a reversible HSP90 inhibitor with a K_d value of 280 nM for the N-terminal ATP-binding domain of purified human Hsp90α. G3130 binds to the adenine site via a multi-hydrogen bond network. G3130 induces the degradation of Hsp90 client protein Her-2 in breast cancer cells. G3130 activates Hsp70 promoter-driven luciferase expression in 293T cells. G3130 can be used in breast cancer-related research.