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

OncoACP3 is a small-molecule ligand of prostatic acid phosphatase (ACP3) with an IC50 of 0.30 nM. OncoACP3 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 is applicable to research related to prostate cancer.

It is advisable to consider the salt form (OncoACP3 TFA) that retains the same biological activity.

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

OncoACP3

OncoACP3 Chemical Structure

CAS No. : 3084147-81-6

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Description

OncoACP3 is a small-molecule ligand of prostatic acid phosphatase (ACP3) with an IC50 of 0.30 nM. OncoACP3 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 is applicable to research related to prostate cancer[1].

In Vitro

OncoACP3 binds to human recombinant ACP3 with ultra-high affinity, with a dissociation rate of 1.2 × 10-4 s-1[1].
177Lu-OncoACP3 specifically binds to HT1080.hACP3 and PC3.hACP3 cells expressing ACP3, but does not bind to ACP3-negative wild-type cells[1].
177Lu-OncoACP3 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) induces potent antitumor activity and even complete cure in tumor-bearing mice[1].
OncoACP3 is conjugated to the cytotoxic agent MMAE (HY-15162) via a cleavable linker to construct the small-molecule drug conjugate OncoACP3-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.

Molecular Weight

1209.33

Formula

C60H81N12O13P

CAS No.
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

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Please store the product under the recommended conditions in the Certificate of Analysis.

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  • 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.

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OncoACP3
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HY-175023
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