Folate Receptor (FR) Ligand

Ricorfotide vedotin (CBP-1008) is a dual-ligand peptide-drug conjugate (PDC) conjugated to MMAE (HY-15162), targeting Folate receptor α (FRα) and TRPV6. Ricorfotide vedotin binds to FRα with high affinity and TRPV6 with low affinity. Ricorfotide vedotin has antitumor activity, and can be used in advanced solid tumor research (eg: colorectal cancer, breast cancer, non-small cell lung cancer, ovarian cancer, adrenocortical carcinoma and follicular dendritic cell sarcoma).

DBCO-PEG1000-FA (DBCO-PEG1000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications.

CBP-1018 is a PDC (peptide-drug conjugate) formed by conjugating Monomethyl auristatin E (HY-15162) to a dual-targeting ligand of FLOR1/PSMA (prostate-specific membrane antigen) via a linker (HY-78738). CBP-1018 binds to FLOR1 and prostate-specific membrane antigen (PSMA). CBP-1018 is applicable to the research of solid tumors and metastatic castration-resistant prostate cancer.

DBCO-PEG-FA (DBCO-PEG-Folate) (MW 3400) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications.

DBCO-PEG10000-FA (DBCO-PEG10000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications.

DBCO-PEG2000-FA (DBCO-PEG2000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications.

DBCO-PEG5000-FA (DBCO-PEG5000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications.

AZD5335 is an ADC targeting FRα, with an IC₅₀ of 10.6 nM against human FRα. AZD5335 specifically binds to FRα, mediates internalization and trafficking to lysosomal compartments, while delivering a topoisomerase I inhibitor payload that traps TOP1-DNA cleavage complexes. AZD5335 induces DNA damage response via the ATR, ATM, Chk1 and Chk2 signaling pathways, and increases the levels of phosphorylated KAP1, phosphorylated RPA, phosphorylated γH2AX, as well as PARP cleavage. AZD5335 exhibits bystander cytotoxicity against FRα-negative cells co-cultured with FRα-expressing cells. AZD5335 induces potent and durable responses and complete regression in ovarian cancer models, including models with low FRα expression and models resistant to Elahere, with enhanced efficacy when combined with Carboplatin, Bevacizumab or poly (ADP-ribose) polymerase inhibitors. AZD5335 can be used for ovarian cancer research.