EGFR Ligand

Camelliaside A is a phytochemical and also a HER2 ligand. Camelliaside A shows no inhibitory effect on mycelial growth of Rhizoctonia solani, indicating no antifungal activity against this pathogen. Camelliaside A is applicable to breast cancer-related research.

FAAH-IN-2 (O-Desmorpholinopropyl Gefitinib) is an inhibitor of FAAH. FAAH-IN-2 is a metabolite of Gefitinib (HY-50895).

(+)-Theta-cypermethrin is a stereoisomer of Cypermethrin (HY-B0829) that possesses blood-brain barrier penetration ability and binds to AKT1, SRC, STAT3 and EGFR with high affinity. (+)-Theta-cypermethrin reduces the amplitude of delayed rectifier potassium channel currents, shifts the steady-state activation curve to negative potentials, and shifts the steady-state inactivation curve to negative potentials at higher concentrations. (+)-Theta-cypermethrin induces abnormal electrical activity in rat hippocampal neurons. (+)-Theta-cypermethrin causes chronic respiratory system damage and exhibits neurotoxicity.

WGYRGFYC (WC8) is a selective HER2-targeting peptide that binds specifically to HER2 by mimicking the antigen-binding site of trastuzumab. The DOTA precursor of WGYRGFYC has a K_D of 61.20 nM for HER2. WGYRGFYC enables specific and highly sensitive detection of HER2 expression in HER2-positive breast cancer cells and tumor tissues, and monitors the dynamic downregulation of HER2 expression. WGYRGFYC rapidly distributes to target tissues and is efficiently cleared from non-target tissues via the kidneys, generating an ideal tumor-to-background ratio in imaging; it is a component of the PET radiotracer Ga-DOTA-WC8. WGYRGFYC exhibits no significant cytotoxicity in breast cancer cells, and can be used for non-invasive imaging diagnosis and therapeutic efficacy evaluation of HER2-positive breast cancer.

Brigatinib A is an GID4 ligand. Brigatinib A can be used for synthesizing PROTAC BCR-ABL Degrader-2 (HY-174368).

EGFR Ligand-Linker Conjugates 4 is a conjugate of the EGFR ligand (HY-178313) and the linker. EGFR Ligand-Linker Conjugates 4 can be used for synthesizing PROTAC EGFR degrader 16 (HY-178242).

HER2-targeted peptide H10 is a HER2-targeting peptide with a K_d value of 30.4 nM. HER2-targeted peptide H10 specifically accumulates in HER2-positive tumor tissues of xenograft mice, when conjugated with nanoparticles. HER2-targeted peptide H10 can be used for studies related to HER2-positive breast cancer.

DOTA-WC8 is a HER2-targeting peptide probe with a K_D of 61.20 nM. ⁶⁸Ga-labeled DOTA-WC8 serves as a PET imaging agent for the specific identification of HER2-positive breast cancer. DOTA-WC8 is applicable to breast cancer-related research.

DL149 is a component of an antibody-drug conjugate (ADC) formed by conjugating the eIF4A inhibitor FD236 (HY-186186) with an ADC linker, and exhibits potential antitumor activity. DL149 can bind to an anti-HER2 antibody to form a complete ADC molecule, which precisely binds to the HER2 receptor on the surface of tumor cells. After internalization into cells, it releases the eIF4A inhibitor payload. DL149 irreversibly blocks the mRNA translation process in tumor cells, thereby inhibiting tumor cell proliferation and inducing their death. DL149 exhibits in vivo antitumor activity in the SK-OV-3 xenograft tumor model, and can be used for the research of HER2-positive solid tumors.

SG3376 is an antibody-drug conjugate (ADC) targeting human epidermal growth factor receptor 2 (HER2). SG3376 is promising for research of HER2-overexpressing cancers (e.g., breast, gastric cancer).

EGFR ligand-20 is a EGFR-binding ligand that serves as a target protein ligand for ZSH-2117 (HY-174415) and is used in studies related to PROTAC synthesis.

Cyclo (KLARLLT) is an EGFR ligand with a K_d value of 1.16 μM. Cyclo (KLARLLT) binds to domain I of EGFR and interacts with both the open and closed conformations of EGFR. Cyclo (KLARLLT) is a modified variant of LARLLT (HY-P11078). Cyclo (KLARLLT) can be used in the research of colorectal cancer.

Tucatinib analog B is a HER2 ligand and a derivative of Tucatinib (HY-16069). Tucatinib analog B can be used in the synthesis of PROTAC degraders, such as serving as the target protein ligand for PROTAC HER2 degrader-1 (HY-177008). Tucatinib analog B is applicable to studies related to HER2-positive cancers.

HYNIC-H6F is a SPECT imaging probe with binding specificity for human epidermal growth factor receptor 2 (HER2) domain II (IC₅₀ = 11 nM). HYNIC-H6F accumulates in HER2-positive breast cancer xenografts via receptor-mediated uptake, while shows low uptake in HER2-negative breast cancer xenografts. HYNIC-H6F enables non-invasive detection of HER2-positive breast cancer in mouse models and allows evaluation of HER2 expression levels without blocking interference. HYNIC-H6F can be used in breast cancer-related research.

Cyclo[K(N3)larllt] is a seven-membered cyclic peptide targeting EGFR, with a K_d value of 5.09 μM, and exhibits binding selectivity toward homologous proteins HER2 and HER3. Cyclo[K(N3)larllt] has no cytotoxicity and shows no growth inhibitory effect on cancer cells overexpressing EGFR. Cyclo[K(N3)larllt] can serve as a ligand for EGFR-targeted fluorescent conjugates, which is applicable to the detection of cancers with EGFR overexpression. Cyclo[K(N3)larllt] can be used in the research of colorectal cancer.

HYNIC-H10F is a conjugate of HER2-targeting peptide H10F and bifunctional chelator HYNIC. HYNIC-H10F can be used in breast cancer-related research.

NSC 104999 is a Grb7 SH2 domain binder with moderate affinity (K_d = 32.3 μM). NSC 104999 exhibits anticancer activity against breast cancer.