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Vipivotide tetraxetan (PSMA-617) Drug-Linker Conjugates for ADC inhibitor

Name: Vipivotide tetraxetan (PSMA-617)
Brand: Selleck Chemicals
SKU: S8670
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S8670

Vipivotide tetraxetan (PSMA-617) is a chemically modified PSMA(prostate-specific membrane antigen) inhibitor with a Ki of 0.37 nM.

Chemical Structure

Molecular Weight: 1042.14

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Batch: S867001 Water]100 mg/mL]false]]]false]]]false Purity: 99.73%

99.73

Related Targets	Others Dyes Antineoplastic and Immunosuppressive Antibiotics ADC Cytotoxin PROTAC Selection Antibiotics for Transfected Cell Antibiotics for Mammalian Cell Culture ADC Linker Antibiotics for Plant Cell Culture PROTAC Linker Hydrotropic Agents Antibody-Drug Conjugate E3 ligase Ligand Target Protein Ligand Molecular Glues Enzyme Substrate Surfactant Chelating Agent

Chemical Information, Storage & Stability

Molecular Weight	1042.14	Formula	C₄₉H₇₁N₉O₁₆	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1702967-37-0	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1CC(CCC1CNC(=O)CN2CCN(CCN(CCN(CC2)CC(=O)O)CC(=O)O)CC(=O)O)C(=O)NC(CC3=CC4=CC=CC=C4C=C3)C(=O)NCCCCC(C(=O)O)NC(=O)NC(CCC(=O)O)C(=O)O

Solubility

In vitro
Batch:

Water : 100 mg/mL

Molarity Calculator

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In vivo
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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Mechanism of Action

Targets/IC₅₀/Ki	PSMA ^[1] (Cell-free assay) 0.37 nM(Ki)
In vitro	PSMA-617 demonstrates high radiolytic stability for at least 72 h. A high inhibition potency (equilibrium dissociation constant Ki = 2.34 ± 2.94 nM on LNCaP; Ki = 0.37 ± 0.21 nM enzymatically determined) and highly efficient internalization into LNCaP cells are demonstrated.^[1]
In vivo	The small-animal PET measurements show high tumor-to-background contrasts as early as 1 h after injection. In vivo distribution reveals specific uptake in LNCaP tumors and in the kidneys 1 h after injection. With regard to therapeutic use, PSMA-617 exhibits a rapid clearance from the kidneys from 113.3 ± 24.4 at 1 h to 2.13 ± 1.36 percentage injected dose per gram at 24 h. The favorable pharmacokinetics of the molecule leads to tumor-to-background ratios of 1,058 (tumor to blood) and 529 (tumor to muscle), respectively,24 h after injection.^[1]
References	[1] https://pubmed.ncbi.nlm.nih.gov/25883127/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06303713	Not yet recruiting	Prostate Cancer\|Metastatic Prostate Cancer\|Metastatic Castration-resistant Prostate Cancer	Dana-Farber Cancer Institute\|Novartis	May 2024	Phase 1
NCT06004661	Recruiting	Metastatic Castration-Resistant Prostate Cancer (mCRPC)	Novartis Pharmaceuticals\|Novartis	April 4 2024	Phase 2
NCT05766371	Recruiting	Castrate Resistant Prostate Cancer\|Metastatic Castration-resistant Prostate Cancer\|Prostate Cancer\|Prostate Carcinoma	University of California San Francisco\|Merck Sharp & Dohme LLC\|Prostate Cancer Foundation	December 15 2023	Phase 2
NCT05228106	Recruiting	Solid Cancers	Centre de recherche du Centre hospitalier universitaire de Sherbrooke	January 21 2022	--

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