2. Antibody-drug Conjugate/ADC Related
  3. Drug-Linker Conjugates for ADC
  4. Vipivotide tetraxetan

Vipivotide tetraxetan  (Synonyms: PSMA-617)

製品番号: HY-117410 純度: 99.46%
COA 取扱説明書 Technical Support

Vipivotide tetraxetan (PSMA-617) is a high potent prostate-specific membrane antigen (PSMA) inhibitor, with a Ki of 0.37 nM. Vipivotide tetraxetan (PSMA-617) is designed consisting of three components: the pharmacophore Glutamate-urea-Lysine, the chelator DOTA able to complex both 68Ga or 177Lu, and a linker connecting these two entities. Glutamate-urea-Lysine is the selective pharmacophore to bind to prostate specific membrane antigen.

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CAS 番号 : 1702967-37-0

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 1432 在庫あり
Solution
10 mM * 1 mL in DMSO USD 1432 在庫あり
Solid
1 mg $234 在庫あり
2 mg $350 在庫あり
5 mg $770 在庫あり
10 mg $1250 在庫あり
50 mg $2300 在庫あり
100 mg $2990 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 17 publication(s) in Google Scholar

Vipivotide tetraxetan 関連抗体

Top Publications Citing Use of Products

    Vipivotide tetraxetan purchased from MedChemExpress. Usage Cited in: J Nucl Med. 2025 Apr 1;66(4):599-604.  [Abstract]

    177Lu-Vipivotide tetraxetan (PSMA-617) (30 MBq) significantly suppressed tumor growth from day 18 to day 35 and was well tolerated in the LNCaP xenograft-bearing mice, and no significant weight loss was noted.

    Vipivotide tetraxetan purchased from MedChemExpress. Usage Cited in: Eur J Nucl Med Mol Imaging. 2025 Apr;52(5):1671-1684.  [Abstract]

    Representative torso MIP, CT, and PET/CT imaging with [68Ga]Ga-NYM032 and [68Ga]Ga-Vipivotide tetraxetan (PSMA617) (111 MBq/patient) were performed on the same PCa patients. [68Ga]Ga-Vipivotide tetraxetan (PSMA617) showed good diagnostic efficiency for primary, recurrent, and metastatic PCa lesions.

    Vipivotide tetraxetan purchased from MedChemExpress. Usage Cited in: Biosens Bioelectron. 2024 Mar 1:247:115956.  [Abstract]

    SPECT scans show progression of 177Lu-Vipivotide tetraxetan (PSMA-617) (i.v.) activity accumulation in PC3-PIP and PC3-flu tumors at five time points taken at the end of every custom γ-probe recording.

    Vipivotide tetraxetan purchased from MedChemExpress. Usage Cited in: Eur J Nucl Med Mol Imaging. 2023 Jul;50(8):2342-2352.  [Abstract]

    Representative SPECT images and biodistribution of HepG2 tumor-bearing mice injected with [177Lu]Lu-Vipivotide tetraxetan (PSMA-617) (37 MBq). Tumor uptake of [177Lu]Lu- Vipivotide tetraxetan (PSMA-617) decreased over time indicating rapid blood clearance and short tumor retention time.

    Vipivotide tetraxetan purchased from MedChemExpress. Usage Cited in: Eur J Nucl Med Mol Imaging. 2023 Jul;50(8):2342-2352.  [Abstract]

    Efficacy of radioligand therapy of HepG2 tumor-bearing mice models injected with a single dose of [177Lu]Lu-Vipivotide tetraxetan (PSMA-617) (37 MBq) and [177Lu]Lu-EB-Vipivotide tetraxetan (PSMA-617). Treatment groups exhibited significantly reduced tumor volume and weight compared with the saline group.

    Drug-Linker Conjugates for ADC アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    Auristatin Camptothecins Daunorubicins/Doxorubicins Duocarmycins Maytansinoids Pyrrolobenzodiazepines Traditional Cytotoxic Agents Dual payloads

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    製品説明

    Vipivotide tetraxetan (PSMA-617) is a high potent prostate-specific membrane antigen (PSMA) inhibitor, with a Ki of 0.37 nM. Vipivotide tetraxetan (PSMA-617) is designed consisting of three components: the pharmacophore Glutamate-urea-Lysine, the chelator DOTA able to complex both 68Ga or 177Lu, and a linker connecting these two entities. Glutamate-urea-Lysine is the selective pharmacophore to bind to prostate specific membrane antigen.

    IC50 & Target

    Traditional Cytotoxic Agents

     

    体外実験

    Vipivotide tetraxetan (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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Vipivotide tetraxetan 関連抗体
    体内実験

    Organ distribution with 68Ga-labeled Vipivotide tetraxetan (PSMA-617) after 1 h (n=3) reveals a high specific uptake in LNCaP tumors and in the kidneys. The high uptake in the kidneys is nearly completely blocked by coinjection of 2 mg of 2-PMPA per kilogram. Other organs such as the liver, lung, and spleen show rather low uptake and no blocking effect, with the exception of the spleen. Tumor-to-background ratios are 7.8 (tumor to blood) and 17.1 (tumor to muscle) at 1 h after injection. As compared with the 68Ga-labeled version, the organ distribution with 177Lu-labeled Vipivotide tetraxetan (PSMA-617) (n=3) show a similar uptake in the LNCaP tumors and in the kidneys. The liver uptake is found to be statistically different. Tumor-to-background ratios determined 1 h after injection show slightly higher values (tumor to blood, 22.1; tumor to muscle, 25.6) than previous organ distribution with 68Ga-labeled Vipivotide tetraxetan (PSMA-617)[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    1042.14

    分子式

    C49H71N9O16
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(O)[C@H](CCCCNC([C@H](CC1=CC=C2C=CC=CC2=C1)NC([C@H]3CC[C@H](CNC(CN4CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC4)=O)CC3)=O)=O)NC(N[C@H](C(O)=O)CCC(O)=O)=O
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 100 mg/mL (95.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : ≥ 100 mg/mL (95.96 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

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    体積 （終了）

    V2

    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (2.00 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (2.00 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    純度とドキュメンテーション

    純度: 99.46%

    COA (247 KB) HNMR (334 KB) RP-HPLC (275 KB) MS (68 KB)

    取扱説明書 (2659 KB)
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 0.9596 mL 4.7978 mL 9.5956 mL 23.9891 mL
    5 mM 0.1919 mL 0.9596 mL 1.9191 mL 4.7978 mL
    10 mM 0.0960 mL 0.4798 mL 0.9596 mL 2.3989 mL
    15 mM 0.0640 mL 0.3199 mL 0.6397 mL 1.5993 mL
    20 mM 0.0480 mL 0.2399 mL 0.4798 mL 1.1995 mL
    25 mM 0.0384 mL 0.1919 mL 0.3838 mL 0.9596 mL
    30 mM 0.0320 mL 0.1599 mL 0.3199 mL 0.7996 mL
    40 mM 0.0240 mL 0.1199 mL 0.2399 mL 0.5997 mL
    50 mM 0.0192 mL 0.0960 mL 0.1919 mL 0.4798 mL
    60 mM 0.0160 mL 0.0800 mL 0.1599 mL 0.3998 mL
    80 mM 0.0120 mL 0.0600 mL 0.1199 mL 0.2999 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Vipivotide tetraxetan Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質量   濃度   体積   分子量 *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Vipivotide tetraxetan1702967-37-0PSMA-617PSMA617PSMA 617Drug-Linker Conjugates for ADCInhibitorinhibitorinhibit

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    製品名:
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    製品番号:
    HY-117410
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