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| CAS:139570-93-7:Zoptarelin doxorubicin | |
| Zoptarelin doxorubicin is a peptide-drug conjugate (PDC). It uses a high-affinity LHRH agonist peptide as the targeting carrier to directionally deliver the cytotoxic drug doxorubicin to tumor cells with high LHRH receptor expression (prostate cancer, breast cancer, endometrial cancer), and releases the drug inside the tumor to exert killing effect, significantly reducing the systemic toxic side effects of chemotherapeutic drugs. Applied in targeted antitumor research, peptide drug conjugation technology, and reproductive system tumor targeted therapy research. | |
| 90%/95%/98% | |
| ~1700 (subject to actual batch) | |
| Peptide-small molecule conjugate, cleavable linker |
| Function Tags (comma-separated) | ||||||||
| Zoptarelin doxorubicin; LHRH-targeted doxorubicin conjugate; AN-152 | Targeted antitumor,Peptide-drug conjugate,LHRH receptor targeting,Prostate cancer research,Reduced chemotherapy toxicity,Reproductive system tumors | LHRH agonist decapeptide + cleavable linker + doxorubicin anthracycline pharmacophore | Large conjugate, no precise small-molecule formula; subject to actual batch MS | - | ~1700 (theoretical) | Peptide-small molecule conjugate |
| Long-term Storage Conditions | Short-term Storage Conditions | ||||
| PEP-ZOP001 | Orange-red powder | Store at -20℃, strictly protected from light, sealed and dry, aliquoted. **Cytotoxic, handle with protection** | Solid powder stable for 1 year at 2-8℃ sealed in dark; prepare aqueous solutions freshly before use | Stable for 48 h at 4℃ in dark; stable for 2 weeks at -20℃ in aliquots. **Moderate water solubility, freely soluble in aqueous organic solvents and acidic buffers**. Anthracycline structure highly sensitive to light and prone to oxidative degradation. Linker easily cleaved under acid/base and enzymatic conditions to release drug | Stable for 2 years at -20℃ under dry & dark conditions |
| Applicable Research Areas (comma-separated) | ||||
| PEP-ZOP001 | LHRH-targeted peptide-drug conjugate that directionally delivers doxorubicin to kill tumors and reduces systemic chemotherapy toxicity | Zoptarelin doxorubicin is a classic targeted peptide-drug conjugate, formed by conjugating LHRH agonist peptide with doxorubicin via a cleavable linker. Its targeting carrier peptide binds with high specificity to LHRH receptors highly expressed on the surface of tumor cells, mediates endocytosis of the conjugate into cells, and the linker is cleaved under the action of intracellular acidic environment and enzymes, releasing active doxorubicin, which intercalates into DNA and inhibits topoisomerase II, blocking nucleic acid synthesis and inducing tumor cell apoptosis. Compared with free doxorubicin, it significantly increases the drug concentration at the tumor site, reduces drug exposure to normal tissues such as heart and bone marrow, and significantly reduces toxic side effects. This molecule serves as a core tool for peptide drug conjugation technology research, reproductive system tumor targeted therapy, and chemotherapy toxicity reduction protocol optimization. | Gonadotropin-Releasing Hormone Receptor (GnRHR/LHRHR); Topoisomerase II inhibition; DNA damage and tumor cell apoptosis pathway |
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