FAPI-X5
FAPI-X5 is a fibroblast activation protein (FAP) inhibitor. FAPI-X5 binds to the FAP catalytic domain, forming hydrogen bonds with key active residues and engaging in π-π stacking to drive functional inhibition. FAPI-X5 exhibits albumin binding activity to prolong systemic circulation half-life. FAPI-X5 induces cytostatic effects on glioblastoma tumors, slowing tumor growth without regression. FAPI-X5, when labeled with 68Ga, acts as a PET tracer with rapid tumor uptake and high-contrast imaging in glioblastoma tumor-bearing mice. FAPI-X5, when labeled with 177Lu or 47Sc, functions as a targeted radionuclide agent with prolonged tumor retention. FAPI-X5 can be used for the research of glioblastoma.
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- No. CAS: 3056070-96-0
- Fòrmula: C63H88F2IN15O13
- Peso molecular:1428.37
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
FAPI-X5 (10 μg) when radiolabeled with 68Ga, 177Lu, or 47Sc exhibits >95% radiochemical purity, >40% albumin binding, and high in vitro stability, with 68Ga-FAPI-X5 showing the highest hydrophilicity and 177Lu- and 47Sc-FAPI-X5 showing slightly higher albumin binding[1].
FAPI-X5 (30-240 min) when radiolabeled with 68Ga, 177Lu, or 47Sc exhibits time-dependent cellular uptake in FAP-expressing U87MG cells, with 68Ga-FAPI-X5 showing the highest uptake at 2 h, and all variants reaching peak uptake by 4 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:U87MG tumor-bearing mice[1]
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Dosage:18.5 MBq, 37 MBq, 55.5 MBq
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Administration:I.v.; single dose
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Result:Produced cytostatic effects with T/C values of 35.49% ± 3.8% at 18.5 MBq, 46.1% ± 4.7% at 37 MBq, and 57.2% ± 5.3% for 177Lu-FAPI-X5.
Produced cytostatic effects with T/C values of 37.50% ± 2.7% at 18.5 MBq, 36.8% ± 3.2% at 37 MBq, and 42.8% ± 3.6% for 47Sc-FAPI-X5.
Caused dose-dependent body weight loss, with a maximum loss of 11% at the 55.5 MBq 47Sc-FAPI-X5 dose, plateauing by day 10.
Resulted in one death in the 37 MBq 47Sc-FAPI-X5 group and one in the 55.5 MBq 177Lu-FAPI-X5 group.
Induced centrilobular coagulative necrosis of hepatocytes, ulcerative necrosis of intestinal mucosa, and mild inflammatory cell infiltration in cardiac and renal tissues.
Chemical Information
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No. CAS 3056070-96-0
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Peso molecular 1428.37
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Fòrmula C63H88F2IN15O13
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SMILES
OC(CN1CCN(CC(O)=O)CCN(CC(NCCCC[C@H](NC(CCCC2=CC=C(I)C=C2)=O)C(N[C@@H](CCCNC(N)=N)C(N3CCC(CCCOC4=CC=C(N=CC=C5C(NCC(N6CC(F)(F)C[C@H]6C#N)=O)=O)C5=C4)CC3)=O)=O)=O)CCN(CC(O)=O)CC1)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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