| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Vipivotide tetraxetan (also known as PSMA-617) is a novel and highly potent prostate-specific membrane antigen (PSMA) inhibitor with anticancer activity. It inhibits PSMA with a Ki of 0.37 nM. Vipivotide tetraxetan is a ligand used to make 177Lu-PSMA-617 [Pluvicto (lutetium (177Lu) vipivotide tetraxetan)], which is a radioactive molecule approved in 2022 to combat cancer. PSMA-617 originally was developed at the German Cancer Research Center and the Heidelberg University Hospital. ABX held the exclusive license to bring the treatment through early clinical development.
| Targets |
Traditional Cytotoxic Agents
|
|---|---|
| ln Vitro |
For a minimum of 72 hours, pipivotide tetraxetan (PSMA-617) exhibits high radiolytic stability. It is shown to have a high inhibition potency (equilibrium dissociation constant Ki=2.34±2.94 nM on LNCaP; determined enzymatically to be Ki=0.37±0.21 nM) and to internalize into LNCaP cells very efficiently[1].
|
| ln Vivo |
After 1 hour (n = 3), organ distribution with 68Ga-labeled Vipivotide tetraxetan (PSMA-617) reveals a high specific uptake in the kidneys and LNCaP tumors. By coinjecting 2 mg of 2-PMPA per kilogram, the high uptake in the kidneys is almost entirely blocked. Except for the spleen, other organs like the liver, lung, and spleen exhibit relatively low absorption and no blocking effect.At one hour following injection, the tumor-to-background ratios are 7.8 (tumor to blood) and 17.1 (tumor to muscle). The organ distribution of 177Lu-labeled Vipivotide tetraxetan (PSMA-617) (n=3) demonstrates a similar uptake in the kidneys and LNCaP tumors as compared to the 68Ga-labeled version. It is discovered that the liver uptake differs statistically. Tumor-to-background ratios measured one hour after injection reveal somewhat higher values than the prior organ distribution with 68Ga-labeled Vipivotide tetraxetan (PSMA-617)[1]. Tumor to blood is 22.1, and tumor to muscle is 25.6.
|
| References |
| Molecular Formula |
C49H71N9O16
|
|---|---|
| Molecular Weight |
1042.1388
|
| Exact Mass |
1,041.50
|
| Elemental Analysis |
C, 56.47; H, 6.87; N, 12.10; O, 24.56
|
| CAS # |
1702967-37-0
|
| Related CAS # |
1702967-37-0;PSMA617 TFA;
|
| PubChem CID |
122706786
|
| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
11
|
| Hydrogen Bond Acceptor Count |
20
|
| Rotatable Bond Count |
27
|
| Heavy Atom Count |
74
|
| Complexity |
1870
|
| Defined Atom Stereocenter Count |
3
|
| InChi Key |
JBHPLHATEXGMQR-LFWIOBPJSA-N
|
| Chemical Name |
(((S)-1-carboxy-5-((S)-3-(naphthalen-2-yl)-2-((1r,4S)-4-((2-(4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl)acetamido)methyl)cyclohexane-1-carboxamido)propanamido)pentyl)carbamoyl)-L-glutamic acid tetra(trifluoroacetic acid)
|
| Synonyms |
PSMA-617; WHO 11010; PSMA617; WHO-11010; PSMA 617; WHO11010;
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~119.95 mM)
H2O : ≥ 100 mg/mL (~95.96 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.00 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (2.00 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (2.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+ 40% PEG300+ 5% Tween-80+ 45% saline: ≥ 2.08 mg/mL (2.00 mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9596 mL | 4.7978 mL | 9.5956 mL | |
| 5 mM | 0.1919 mL | 0.9596 mL | 1.9191 mL | |
| 10 mM | 0.0960 mL | 0.4798 mL | 0.9596 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05682443 | RECRUITING | Drug: ONC-392 | Metastatic Castration- resistant Prostate Cancer |
OncoC4, Inc. | 2023-12-11 | Phase 1 Phase 2 |
| NCT05803941 | RECRUITING | Drug: AAA617 | Prostate Cancer | Novartis Pharmaceuticals | 2023-08-14 | Phase 4 |
| NCT05849298 | RECRUITING | Drug: AAA617 Drug: AAA517 Drug: Piflufolastat F 18 |
Prostatic Neoplasm | Novartis Pharmaceuticals | 2024-01-03 | Phase 2 |
| NCT06099093 | RECRUITING | Drug: 18F-DCFPyl | Prostate Cancer | Brigham and Women's Hospital | 2024-04-01 | Phase 4 |
| NCT05658003 | ACTIVE | Drug: [177Lu]Lu-PSMA-617 Drug: ARDT Drug: [68Ga]Ga-PSMA-11 Other: Best supportive care |
Metastatic Castration-Resistant Prostate Cancer (mCRPC) |
Novartis Pharmaceuticals | 2023-05-05 | Phase 2 |
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
