OncoACP3 TFA
Based on 1 Customer Validation
OncoACP3 TFA is a small-molecule ligand of prostatic acid phosphatase (ACP3) with an IC50 of 0.30 nM. OncoACP3 TFA has a modular structure that supports flexible payload delivery. After radiolabeling with Lu-177 it selectively accumulates in ACP3-expressing tumors with a long retention time, enabling targeted radiation delivery. OncoACP3 TFA is applicable to research related to prostate cancer.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.87%
- 分子式: C62H82F3N12O15P
- 分子量:1323.35
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
体外実験
OncoACP3 TFA binds to human recombinant ACP3 with ultra-high affinity, with a dissociation rate of 1.2 × 10-4 s-1[1].
177Lu-OncoACP3 TFA specifically binds to HT1080.hACP3 and PC3.hACP3 cells expressing ACP3, but does not bind to ACP3-negative wild-type cells[1].
177Lu-OncoACP3 TFA specifically localizes to the membranes of HT1080.hACP3 and PC3.hACP3 cells that express ACP3, but does not bind to wild-type cells without ACP3 expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
体内実験
OncoACP3 TFA is conjugated to the cytotoxic agent MMAE (HY-15162) via a cleavable linker to construct the small-molecule drug conjugate OncoACP3 TFA-GlyPro-MMAE, which enables targeted chemotherapy in mouse models[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic BALB/c AnNRj-Foxn1 nude mice (male, 4-10 weeks old, subcutaneous flank implantation of HT1080.hACP3 cells)[1]
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Dosage:5 MBq per injection (250 MBq/kg); 20 MBq per injection (1,000 MBq/kg)
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Administration:i.v.; single injection
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Result:Induced tumor regression in all treated animals at 5 MBq per injection, with 25% (1/4) complete tumor response by therapy day 31.
Achieved 100% (4/4) complete tumor response at 20 MBq per injection.
Showed good tolerability with no excessive body weight loss observed.
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Animal Model:Athymic BALB/c AnNRj-Foxn1 nude mice (female, 4-10 weeks old, subcutaneous flank implantation of HT1080.hACP3 cells)[1]
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Dosage:62.5 nmol/kg; 125 nmol/kg; 250 nmol/kg; 500 nmol/kg; 1,000 nmol/kg
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Administration:i.v.; single injection
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Result:Reached ~70% of the injected dose per gram (%ID/g) tumor accumulation at 2 hours post-administration at 62.5 nmol/kg, with low kidney uptake of ~3% ID/g.
Maintained high tumor-to-normal organ ratios across all doses.
Showed partial tumor saturation between 250 nmol/kg and 1,000 nmol/kg.
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Animal Model:Athymic BALB/c AnNRj-Foxn1 nude mice (female and male, 4-10 weeks old, subcutaneous flank implantation of HT1080.hACP3 or PC3.hACP3 cells)[1]
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Dosage:62.5 nmol/kg
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Administration:i.v.; single injection
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Result:Exhibited a tumor half-life of ~72 hours in female mice with HT1080.hACP3 tumors.
Showed a tumor half-life exceeding 72 hours in male mice with PC3.hACP3 tumors.
Demonstrated low accumulation in all healthy organs, including salivary glands and reproductive tissues, across all time points.
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Animal Model:Athymic BALB/c AnNRj-Foxn1 nude mice (subcutaneous flank implantation of HT1080.hACP3 or PC3.hACP3 cells)[1]
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Dosage:250 nmol/kg
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Administration:i.v.; repeated injections as scheduled
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Result:Delivered ~150 pmol/g of MMAE to HT1080.hACP3 tumors and ~15 pmol/g of MMAE to PC3.hACP3 tumors at 24 hours post-administration, with minimal MMAE accumulation in healthy organs.
Significantly inhibited tumor growth in both HT1080.hACP3 and PC3.hACP3 tumor models compared to vehicle or non-cleavable OncoACP3-MMAE, with greater efficacy observed in the HT1080.hACP3 model.
化学情報
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性状 Solid
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分子量 1323.35
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分子式 C62H82F3N12O15P
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Color White to off-white
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SMILES
OC(CN1CCN(CC(NCCCCCCNC([C@H]2N(C(CN(CC3=CC=CC=C3)CC4=CC=CC=C4)=O)C[C@@H](N5N=NC(COC6=CC=C(C(NCC7=CC=CC=C7)P(O)(O)=O)C=C6)=C5)C2)=O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC1)=O.OC(C(F)(F)F)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (75.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (1.89 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (1.89 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (283 KB)
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SDS (252 KB)
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- Portuguese - PT (252 KB)
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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 (sealed storage, away from moisture). 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 | 1 mM | 0.7557 mL | 3.7783 mL | 7.5566 mL | 18.8915 mL |
| 5 mM | 0.1511 mL | 0.7557 mL | 1.5113 mL | 3.7783 mL | |
| 10 mM | 0.0756 mL | 0.3778 mL | 0.7557 mL | 1.8891 mL | |
| 15 mM | 0.0504 mL | 0.2519 mL | 0.5038 mL | 1.2594 mL | |
| 20 mM | 0.0378 mL | 0.1889 mL | 0.3778 mL | 0.9446 mL | |
| 25 mM | 0.0302 mL | 0.1511 mL | 0.3023 mL | 0.7557 mL | |
| 30 mM | 0.0252 mL | 0.1259 mL | 0.2519 mL | 0.6297 mL | |
| 40 mM | 0.0189 mL | 0.0945 mL | 0.1889 mL | 0.4723 mL | |
| 50 mM | 0.0151 mL | 0.0756 mL | 0.1511 mL | 0.3778 mL | |
| 60 mM | 0.0126 mL | 0.0630 mL | 0.1259 mL | 0.3149 mL |
OncoACP3 TFA 関連分類
HY-175023A 関連分類
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