Peptide Conjugates

Tezuvotide tetraxetan is an antineoplastic peptide.

Lapemelanotide zapixetan exhibits antineoplastic property.

Lead-lapemelanotide zapixetan is a precursor of lapemelanotide, which can be used in life science research.

Lead-bamzireotide navoxetan is an antineoplastic compound that can be labeled with 121Pb for tumor targeting.

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 α_Vβ₃ with IC₅₀ values of 4.25 μM (α_Vβ₃) and 58.7 μM (α_Vβ₅). BGC0222 possesses the property of inducing neovascularization. BGC0222 exhibits good antiproliferation activity in many tumors.

YYLLVR is an angiotensin-converting enzyme (ACE) inhibitory peptide with an inhibitory rate of 89.10%. YYLLVR has a lower binding energy for ACE of -35.98 kcal/mol. YYLLVR can be used in the study of hypertensive diseases.

Pt(IV)-M13 is a BBB-penetrable 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.

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.

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.

BT1769 is a MT1-MMP-targeted (K_D = 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.

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.

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.

BQ7876 is a probe targeting prostate-specific membrane antigen (PSMA) that contains a DOTA chelator. BQ7876, after being radiolabeled with radionuclide (177Lu), functions in both radionuclide imaging and tumor cell destruction by specifically binding to PSMA. BQ7876 shows potential for research in the field of metastatic castration-resistant prostate cancer (mCRPC). BQ7876 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

BQ7859 is a probe targeting PSMA that contains a NOTA chelator and demonstrates excellent imaging performance. BQ7859 can be labeled with various radionuclides, such as 68Ga, 18F, 55Co, and 111In. In a mouse prostate cancer xenograft model, BQ7859 (labeled with 111In) efficiently accumulates in tumor regions in a PSMA-dependent manner and provides high-contrast tumor imaging. BQ7859 shows potential for research in prostate cancer imaging, particularly in positron emission tomography (PET) and single-photon emission computed tomography (SPECT). BQ7859 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

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.

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.

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.

DOTA Conjugated JM#21 derivative 7 (compound Ligand-7) is a derivative of CXCR4 targeting peptide conjugated with DOTA and can be used to produce radioligands. Radiolabeled DOTA Conjugated JM#21 derivative 7, i.e., 177Lu-DOTA, has excellent CXCR4 tumor targeting. In vitro biodistribution results of 177Lu-DOTA showed very low uptake in all non-targeted organs except kidney. DOTA Conjugated JM#21 derivative 7 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

Hynic-toc (HYNIC-Tyr3-octreotide), a octreotide derivative, can be conjugated with radioactive element for tumor imaging. Hynic-toc can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

DOTA-Octreotide is composed of chelator DOTA and Octreotide (HY-P0036). DOTA-Octreotide is used for research of cancer, through combination with radioactive elements. DOTA-Octreotide can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).