Peptide Conjugates

Alkyne-βAG-TOCA, an octreotide derivative, targets somatostatin receptor type 2 (SST2). Alkyne-βAG-TOCA can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

HYNIC-iPSMA TFA is a PSMA-targeted ligand for tumor molecular imaging, with a K_i value of 3.11 nM. HYNIC-iPSMA TFA consists of two components: HYNIC (6-hydrazinonicotinamide) and iPSMA (Inhibitor of Prostate-Specific Membrane Antigen). HYNIC serves as a chelating moiety to link radionuclides to the targeting molecule; iPSMA is a specific inhibitor that targets Prostate-Specific Membrane Antigen (PSMA). 68Ga-labeled iPSMA is used for prostate cancer detection via PET imaging, while the further developed ^99mTc-EDDA/HYNIC-iPSMA TFA exhibits excellent specificity and sensitivity. HYNIC-iPSMA TFA can be used for the synthesis and research of radionuclide-conjugated drugs (RDC).

DOTA-LM3 TFA is a somatostatin receptor (SSTR) antagonist. LM3 refers to p-Cl-Phe- cyclo(D-Cys-Tyr-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr- NH2, as well as a somatostatin antagonist. DOTA-LM3 TFA is often isotopically labeled for tracing tumors in vivo, such as 177Lu-DOTA-LM3 TFA and 68 Ga-DOTA-LM3 TFA. 68 Ga-DOTA-LM3 TFA shows favorable biodistribution, high tumor uptake, good tumor retention, and few safety concerns. 177Lu-DOTA-LM3 TFA can be used for research in DOTATOC-negative liver metastases, such as pancreatic NET and extensive tumor thrombosis. DOTA-LM3 (TFA) can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

Betiatide, as a chelating agent for Technetium-99m (^99mTc), is used to prepare ^99mTc-MAG3 (mercaptoacetyltriglycine), a radiopharmaceutical for renal function imaging. Betiatide is used for the diagnosis of congenital and acquired abnormalities, renal failure, urinary tract obstructions, and calculi. Betiatide can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

c(avb6)-DOTA TFA is a conjugate of the αvβ6 integrin selective peptide ring modified with DOTA chelator. The Lu(III) complex of c(avb6)-DOTA TFA has a comparable affinity for αvβ6 integrin (IC₅₀=0.8 nM) and can be used as a tumor diagnostic.

DOTA-Bombesin (1-14) TFA is composed of chelator DOTA and Bombesin (HY-P0195). DOTA-Bombesin (1-14) TFA is used for research of cancer through combination with radioactive elements. DOTA-Bombesin (1-14)TFA can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

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).

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).

NVP-EVS459 is a Folate Receptor (FR)-targeting radioconjugate. NVP-EVS459 labeled with 177Lu can be used for tumor diagnosis and research.

PSMA-D5 has a binding affinity for PSMA with a K_i of 0.21 nM and can be used for PSMA tracing after radiolabeling. PSMA-D5 ([68Ga]-labeled) contains a DOTA chelator, allowing convenient labeling with therapeutic radionuclides such as 177Lu and 225Ac. PSMA-D5 ([68Ga]-labeled) shows excellent pharmacokinetic properties, exhibiting remarkable tumor uptake in 22Rv1 tumors. PSMA-D5 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

TAT-PiET-PROTAC is a proteolysis-targeting chimera (PROTAC)-modified TAT-PiET (HY-P10445), which is a cell-penetrating peptide targeting the extra-terminal (ET) domain of BRD4. TAT-PiET-PROTAC can reduce BRD4 and JMJD6 levels and inhibit cell proliferation. TAT-PiET-PROTAC also resists the endocrine resistance of ERα-positive breast cancer cells. TAT-PiET-PROTAC can be used for the research of cancer, such as breast cancer.

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.

PDI2 (PSMA-DOTA-PEI2) is a prostate-specific membrane antigen (PSMA) ligand that acts as a tumor retention agent, renal uptake reducer, imaging agent and antitumor agent, applicable in SPECT diagnostic imaging and radiotheranostics. PDI2 specifically binds to PSMA on prostate cancer cells, enters cells via clathrin-dependent endocytosis, and exhibits higher tumor retention rate and lower renal uptake level. PDI2 is applicable in research related to prostate cancer and castration-resistant metastatic prostate cancer.

Pentetreotide is a diethylenetriaminopentaacetic (DTPA) conjugate of Octreotide (HY-P0036). Pentetreotide is a somatostatin analog that, when labeled with ¹¹¹In, can be used for nuclear medicine imaging. Somatostatin receptor scintigraphy with Pentetreotide is effective in visualizing neuroendocrine tumors, and its metastasis.

Tyr3-Octreotate is a ligand for somatostatin receptor subtype 2 (sst2), with an IC₅₀ value of 1.3 nM against sst2 when labeled with [¹¹¹In-DTPA], and an IC₅₀ value of 1.6 nM against sst2 when labeled with [⁹⁰Y-DOTA]. Radiolabeled Tyr3-Octreotate generates cell-associated radioactivity, and acts as both a tumor growth inhibitor and a tumor cytotoxic agent. When radiolabeled with ¹⁷⁷Lu or ⁹⁰Y, Tyr3-Octreotate serves as a peptide receptor radionuclide therapy (PRRT) analog. Tyr3-Octreotate can be used in studies related to pancreatic tumors.

Tyr3-Octreotate acetate is a somatostatin analog. Tyr3-Octreotate acetate exhibits high uptake into tumor, that is capable to be labeled with radioactive metal and thus exhibits antitumor efficacy. Tyr3-Octreotate acetate can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

NOTA-Pep-1L specifically targets the IL13RA2 receptor for tumor imaging. NOTA-Pep-1L can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

DOTA-PSMA-EB-01 (Compound LNC1003) is a specific inhibitor of PSMA (IC₅₀= 10.77 nM).DOTA-PSMA-EB-01 enhances the uptake and retention time of ¹⁷⁷Lu in tumors. DOTA-PSMA-EB-01 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

NODAGA-LM3 TFA is a ligand that can cross the blood-brain barrier and targets somatostatin receptor SSTR2 with high affinity (IC₅₀ = 1.3 nM). NODAGA-LM3 TFA does not trigger the internalization of SSTR2 and can inhibit agonist-induced internalization processes. NODAGA-LM3 TFA shows low uptake in normal tissues such as the liver and spleen, but high uptake in the lungs and blood pool. ⁶⁸Ga-labeled NODAGA-LM3 TFA can serve as a PET imaging agent for well-differentiated neuroendocrine tumors, and is applied in studies related to small cell lung cancer and well-differentiated neuroendocrine tumors.

TAT-BH4 (Bcl-xL) localized mainly at the mitochondria, prevents apoptotic cell death. TAT-BH4 (Bcl-xL) is a fusion peptide that combines the N-terminal cysteine conjugated protein transduction domain of HIV TAT protein (amino acids 49 to 57) with the Bcl-xL BH4 peptide. TAT-BH4 can be used for research of diseases caused by accelerated apoptosis.