2. Signaling Pathways
  3. Antibody-drug Conjugate/ADC Related
  4. Peptide-Drug Conjugates (PDCs)

Peptide-Drug Conjugates (PDCs)

ADC-Related Custom Services

Peptide-Drug Conjugates (PDCs)

Peptide-drug conjugates (PDCs) are the next generation of targeted therapeutics drug after antibody-drug conjugate (ADCs) and hold broad prospects in fields such as tumor treatment. PDCs combine peptides selectivity with chemotherapeutic drugs lethality, with the core benefits of enhanced cellular permeability and improved drug selectivity. PDCs consist of three important components: peptides, linkers and cytotoxic payloads. Among them, peptides mainly include homing peptides and cell-penetrating peptides, which can affect the efficiency of drug endocytosis. The ideal peptide should have high affinity, stability, and so on. Cytotoxins is the key to killing tumor cells and has both therapeutic and imaging functions. Cytotoxins for coupling have four requirements as followed: a clear mechanism of action, a small molecular weight, high cytotoxicity and retained anti-tumor activity after chemical coupling to the peptide. The linker needs to connect the peptide and the cytotoxic payload and can be divided into cleavable and non-cleavable types. The choice of linker is crucial and requires consideration of the microenvironment in which the PDC is located to avoid interfering with the binding affinity of the peptide to its receptor and the drug efficacy. The linker must have a certain level of stability to prevent premature and nonspecific drug release[1].

Peptide-Drug Conjugates (PDCs) Related Products (18):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P4073
    ANG1005
    		98.83%
    ANG1005 (Paclitaxel trevatide) is a brain-penetrating peptide-drug conjugate. ANG1005, a taxane derivative, consists of three paclitaxel (HY-B0015) molecules covalently linked to Angiopep-2, designed to cross the blood-brain and blood-cerebrospinal barriers and to penetrate malignant cells via low density lipoprotein receptor-related protein (LRP1) transport system.
    ANG1005
  • HY-P10762
    CBP-1008
    CBP-1008 is a dual-ligand peptide-drug conjugate (PDC) conjugated to MMAE (HY-15162), targeting Folate receptor α (FRα) and TRPV6. CBP-1008 binds to FRα with high affinity and TRPV6 with low affinity. CBP-1008 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).
    CBP-1008
  • HY-P10740
    CBP-1018
    CBP-1018 is a PDC (peptide drug conjugate) consisting of a dual targeting FRα/TRPV6 ligand (blue part) coupled to Monomethyl auristatin E (HY-15162) (red part) via a linker (HY-78738) (black part). CBP-1018 is expected to be used in breast cancer research.
    CBP-1018
  • HY-P10742
    CBX-12
    CBX-12 is a PDC (peptide drug conjugate) that targets tumors in an antigen-independent manner and exhibits antitumor activity. CBX-12 consists of a pH-sensitive peptide (pHLIP), a self-immolating linker, and a topoisomerase 1 (TOP1) inhibitor Exatecan (HY-13631).
    CBX-12
  • HY-P10773
    CTP-amiodarone
    CTP-amiodarone is a cell-penetrating conjugate of cardiomyocyte targeting peptide and Amiodarone (HY-14187). CTP-amiodarone exhibits antiarrhythmic efficacy through block of Na+, K+, Ca2+ channels and β-adrenergic receptors.
    CTP-amiodarone
  • HY-P10760
    PhAc-ALGP-Dox
    PhAc-ALGP-Dox, a peptide-drug conjugate, is a novel anticancer prodrug, with IC50 values ranged from 311 nM to 34.25 μM for TNBC (E0771), normal murine epithelium (HC-11), human TNBC (MDA-MB-231 and MDA-MB-468), human CrC (LS 174T), normal human epithelium (HME-1) cells.
    PhAc-ALGP-Dox
  • HY-P10775
    BT1769
    BT1769 is a MT1-MMP-targeted (KD = 3.35 nM) Bicycle toxin conjugate. BT1769 can be used in the study for osteosarcoma. BT1769 consists of a novel bicyclic targeting peptide that selectively binds MT1-MMP; a cytotoxin MMAE; and an enzymatically cleavable dipeptide linker.
    BT1769
  • HY-16532
    Zoptarelin doxorubicin
    Zoptarelin doxorubicin (AEZS-108; AN-152) is a hybrid anticancer agent, containing Zoptarelin and Doxorubicin. Zoptarelin doxorubicin has been used to research targeting tumors expressing LHRH receptors. Zoptarelin doxorubicin abolishes tumor progression and induces remarkable apoptosis in vitro.
    Zoptarelin doxorubicin
  • HY-P10765
    DTS-108
    DTS-108 is a prodrug of SN38 (HY-13704) (a Topoisomerase I inhibitor). DTS-108 is a conjugate generated by linking SN38 to a human oligopeptide via an esterase sensitive cross-linker. DTS-108 exhibits anti-tumor activity against colorectal, lung, and mammary cancer.
    DTS-108
  • HY-P10782
    Pt(IV)-M13
    Pt(IV)-M13 is a BBB-penatrable Platinum (IV) prodrug-perfluoroaryl macrocyclic peptide conjugate. Pt(IV)-M13 is cytotoxic to glioma stem cells and increases uptake of platinum in the brain. Pt(IV)-M13 can be used in the study of glioblastoma.
    Pt(IV)-M13
  • HY-P10757
    DTX-P7
    DTX-P7 is a peptide-drug conjugate. DTX-P7, composed of Docetaxel (DTX, HY-B0011) and a heptapeptide (P7), induces unfolded protein response and subsequent apoptosis by degrading Hsp90.
    DTX-P7
  • HY-P10783
    BGC0222
    BGC0222 is a novel prodrug of Irinotecan (HY-16562). BGC0222, as a PEG-cRGD-conjugated Irinotecan (HY-16562) derivative, could slowly and steadily release Irinotecan (HY-16562). BGC0222 binds to αVβ3 with IC50 values of 4.25 μM (αVβ3) and 58.7 μM (αVβ5). BGC0222 possesses the property of inducing neovascularization. BGC0222 exhibits good antiproliferation activity in many tumors.
    BGC0222
  • HY-P10772
    L2P4
    L2P4 is a peptide-based and EBNA1 targeting fluorescent probe, which inhibits the EBNA1 homodimer formation and selectively inhibits EBV+ tumor growth. L2P4 exhibits cytotoxicity in EBV-positive C666-1 cell with LC50 of 46.4 μM.
    L2P4
  • HY-P10759
    DTS-201 sodium
    DTS-201 sodium (CPI-0004Na) is a peptidic prodrug of Doxorubicin (HY-15142A). DTS-201, comprising the tetrapeptide portion, is cleaved by endopeptidases in the tumor environment to produce metabolites that subsequently enter the cell and are converted to active Doxorubicin. DTS-201 shows antitumoral efficacy in tumor xenograft models of prostate, breast, and lung cancer.
    DTS-201 sodium
  • HY-P10698
    VH-N412
    VH-N412 is a vectorized neuropeptide (NT) with good blood-brain barrier permeability. VH-N412 binds to the low-density lipoprotein receptor (LDLR) and neuropeptide receptor 1 (NTSR-1), and acts as a pharmacological-induced hypothermia (PIH) inducer. VH-N412 exhibits anticonvulsant and neuroprotective effects, and can be used in the study of neurological diseases such as epilepsy.
    VH-N412
  • HY-16215
    Mipsagargin
    Mipsagargin (G-202) is a novel thapsigargin-based targeted proagent consisting of a prostate-specific membrane antigen (PSMA)-specific peptide coupled to an analog of the potent sarcoplasmic/endoplasmic reticulum calcium adenosine triphosphatase (SERCA) pump inhibitor Thapsigargin (HY-13433). Mipsagargin is activated by PSMA-mediated cleavage of an inert masking peptide. Mipsagargin has the potential for refractory, advanced or metastatic solid tumours research.
    Mipsagargin
  • HY-P10770
    P-ESBP-DOX
    P-ESBP-DOX is a HPMA copolymer-drug conjugate, which is consistituted of the E-selectin binding peptide and the Doxorubicin (HY-15142). P-ESBP-DOX exhibits cytotoxicity against TNFα-activated human vascular endothelial cells IVECs with an IC50 of 0.28 μM. P-ESBP-DOX can be used in research about tumor vasculature.
    P-ESBP-DOX
  • HY-P10741
    DOTA-EB-TATE
    DOTA-EB-TATE is composed of SST peptide derivative, DOTA-octreotate conjugated a common to an Evans blue analog (EB). DOTA-EB-TATE is a peptide drug conjugate (PDC) improves the pharmacokinetics of SSTR2 analogs and reduces PRRT toxicity. DOTA-EB-TATE can also be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
    DOTA-EB-TATE