1. Immunology/Inflammation
  2. PSMA
  3. PSMA-trillium

PSMA-trillium (Felivotide mopaxetan) is a PSMA-targeted molecule that contains a highly specific PSMA-binding motif, an albumin-binding domain optimized for tumor uptake and retention, and a Macropa chelator conjugated to the α-emitter 225Ac. PSMA-trillium binds to albumin to prolong plasma retention time and binds to PSMA via its specific motif. 225Ac-PSMA-Trillium exhibits dose-dependent inhibition of LNCaP tumor growth in mice. PSMA-trillium can be used in research related to prostate cancer and metastatic castration-resistant prostate cancer.

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

PSMA-trillium

PSMA-trillium Chemical Structure

CAS No. : 3036415-37-6

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Description

PSMA-trillium (Felivotide mopaxetan) is a PSMA-targeted molecule that contains a highly specific PSMA-binding motif, an albumin-binding domain optimized for tumor uptake and retention, and a Macropa chelator conjugated to the α-emitter 225Ac. PSMA-trillium binds to albumin to prolong plasma retention time and binds to PSMA via its specific motif. 225Ac-PSMA-Trillium exhibits dose-dependent inhibition of LNCaP tumor growth in mice. PSMA-trillium can be used in research related to prostate cancer and metastatic castration-resistant prostate cancer[1][2].

In Vitro

225Ac-PSMA-trillium maintains favorable stability for up to 48 h[1].
225Ac-PSMA-trillium (0.114 kBq/mL) potently induces cytotoxicity in C4-2, a subclone of the prostate cancer cell line LNCaP[1].

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

In Vivo

225Ac-PSMA-Trillium (100-400 kBq/kg; intravenous injection; single dose) exhibits dose-dependent inhibition of LNCaP tumor growth and reduces tumor weight in male SCID mice, with higher tumor uptake and faster renal clearance compared to the control agent 225Ac-PSMA-SMOL[2].

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

Animal Model: SCID (male)[2]
Dosage: 100 kBq/kg; 400 kBq/kg
Administration: i.v.; single injection
Result: Showed higher tumor uptake compared to other 225Ac-PSMA-SMOLs, with homogeneous tumor accumulation 60 hours after injection and fast clearance from the kidneys.
Inhibited LNCaP tumor growth and decreased tumor weights in a dose-dependent manner.
Molecular Weight

2371.44

Formula

C106H156IN17O34S

CAS No.
SMILES

O=C([C@@H](NC(N[C@H](C(O)=O)CCCCNC(NC1=CC(C2=CN(N=N2)CCOCCOCCOCCC(N[C@H](C(NCCOCCOCCOCCOCCOCCOCCOCCOCCC(N[C@H](C(O)=O)CCCCNC(CCCC3=CC=C(I)C=C3)=O)=O)=O)CCCCNC(NC4=CC=C(C=C4)CCOC5=CC(C(O)=O)=NC(CN6CCOCCOCCN(CC7=CC=CC(C(O)=O)=N7)CCOCCOCC6)=C5)=S)=O)=CC=C1)=O)=O)CCC(O)=O)O

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

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    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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PSMA-trillium
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HY-158119A
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