1. Metabolic Enzyme/Protease
  2. Phosphatase
  3. OncoACP3 TFA

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.

For research use only. We do not sell to patients.

OncoACP3 TFA

OncoACP3 TFA Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of OncoACP3 TFA:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

In Vitro

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.

In Vivo

177Lu-OncoACP3 (250-1000 MBq/kg, i.v., single administration) TFA induces potent antitumor activity and even complete cure in tumor-bearing mice[1].
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.

Animal Model: Athymic BALB/c AnNRj-Foxn1 nude mice (male, 4-10 weeks old, subcutaneous flank implantation of HT1080.hACP3 cells)[1]
Dosage: 5 MBq per injection (250 MBq/kg); 20 MBq per injection (1,000 MBq/kg)
Administration: i.v.; single injection
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.
Animal Model: Athymic BALB/c AnNRj-Foxn1 nude mice (female, 4-10 weeks old, subcutaneous flank implantation of HT1080.hACP3 cells)[1]
Dosage: 62.5 nmol/kg; 125 nmol/kg; 250 nmol/kg; 500 nmol/kg; 1,000 nmol/kg
Administration: i.v.; single injection
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.
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]
Dosage: 62.5 nmol/kg
Administration: i.v.; single injection
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.
Animal Model: Athymic BALB/c AnNRj-Foxn1 nude mice (subcutaneous flank implantation of HT1080.hACP3 or PC3.hACP3 cells)[1]
Dosage: 250 nmol/kg
Administration: i.v.; repeated injections as scheduled
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.
Molecular Weight

1323.35

Formula

C62H82F3N12O15P

Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.7557 mL 3.7783 mL 7.5566 mL
5 mM 0.1511 mL 0.7557 mL 1.5113 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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: ≥ 2.5 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.
  • Protocol 2

    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:

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.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.87%

References

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 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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
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.

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
OncoACP3 TFA
Cat. No.:
HY-175023A
Quantity:
MCE Japan Authorized Agent: