FZ-AD005
Based on 1 Customer Validation
FZ-AD005 is a DLL3-targeting antibody-drug conjugate (ADC) with high selectivity, composed of the anti-DLL3 antibody FZ-A038 (HY-P990896), a dipeptide linker (Val-Ala), and DXd (HY-13631D). The Kd value of FZ-AD005 for human DLL3 ranges from 13.29 to 58.3 pmol/L. After binding to DLL3 on the cell surface, FZ-AD005 mediates endocytosis, and the payload DXd is released via cleavage by lysosomal cathepsins. DXd inhibits topoisomerase TopI to induce double-strand DNA breaks, cell cycle arrest and apoptosis, and FZ-AD005 exhibits bystander killing activity against adjacent DLL3-negative cells. FZ-AD005 shows stable circulation in vivo, has good tolerance and acceptable pharmacokinetic profiles in rats and cynomolgus monkeys, and effectively inhibits the growth of DLL3-expressing tumor cells. FZ-AD005 serves as a promising candidate molecule for research on small cell lung cancer and human neuroendocrine prostate cancer.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 97.04%
- Peso molecular:154128 (average)
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Almacenamiento:
-80°C, protect from light
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Actividad biológica
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Topoisomerase I |
FZ-AD005 (1 μg/mL; 144 hours) exhibits a strong bystander killing effect, eliminating both DLL3-positive NCI-H82 cells and DLL3-negative Ramos cells in a Transwell coculture system[1].
FZ-AD005 (0.78-100 nmol/L human DLL3) exhibits high affinity binding to human DLL3 (Kd=58.3 pmol/L) and FcRn (Kd=29 nmol/L), but very low affinity for FcγRI, FcγRIIa, and FcγIIIa, when tested in a biolayer interferometry assay[1].
FZ-AD005 (100 μg/mL; 7 days) is highly stable in human plasma, with only ~0.7% DXd released after 7 days of incubation at 37°C[1].
FZ-AD005 (200 pmol; 48 hours) rapidly internalizes into DLL3-expressing cells within 30 minutes, traffics to lysosomes, and releases DXd in a time-dependent manner when tested over 48 hours[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:DLL3-positive NCI-H82 cells, DLL3-negative Ramos cells
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Concentration:1 μg/mL
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Incubation Time:144 hours
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Result:Effectively eliminated both NCI-H82 and Ramos cell populations in the coculture system.
Single intravenous administration of FZ-AD005 (1.5-6 mg/kg; intravenous injection; single dose) at doses of 1.5, 3 and 6 mg/kg induces complete tumor growth inhibition in male NOD/SCID mice inoculated with NCI-H660 NEPC xenografts[1].
FZ-AD005 (1-5 mg/kg; intravenous injection; once weekly; 2 total administrations) induces significant tumor growth inhibition in female BALB/c nude mice bearing NCI-H82 SCLC xenografts; at intravenous doses of 1, 3 and 5 mg/kg given once weekly for 2 total administrations, its TGI ranges from 76.52% to 97.13%[1].
FZ-AD005 (1.5-6 mg/kg; intravenous injection; single administration) induces potent to complete tumor growth inhibition in mice bearing SCLC LU-5236 PDX, with TGIs ranging from 98.51% to 100.00% across different dose groups on day 21 post-administration[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID (female) with Small cell lung cancer[1]
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Dosage:2.5 mg/kg; 5 mg/kg; 10 mg/kg
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Administration:i.v.; single dose
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Result:Achieved tumor growth inhibition (TGI) values of 86.21% (2.5 mg/kg), 94.53% (5 mg/kg), and 95.54% (10 mg/kg) compared to vehicle control.
Caused no obvious body weight loss in treated mice.
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Animal Model:NOD/SCID (male) with Neuroendocrine prostate cancer[1]
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Dosage:1.5 mg/kg; 3 mg/kg; 6 mg/kg
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Administration:i.v.; single dose
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Result:Exhibited complete tumor growth inhibition in all dose groups compared to vehicle control.
Caused no obvious body weight loss in treated mice.
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Animal Model:BALB/c nude (female) with Small cell lung cancer[1]
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Dosage:1 mg/kg; 3 mg/kg; 5 mg/kg
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Administration:i.v.; weekly; 2 total doses
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Result:Achieved tumor growth inhibition (TGI) values of 76.52% (1 mg/kg), 94.19% (3 mg/kg), and 97.13% (5 mg/kg) compared to vehicle control.
Demonstrated notably superior efficacy to lurbinectedin (23.48% TGI at 0.18 mg/kg).
Caused no obvious body weight loss in treated mice.
Chemical Information
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Appearance Liquid
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Peso molecular 154128 (average)
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Color Colorless to light yellow
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SMILES
[FZ-AD005]
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Envío
Shipping with dry ice.
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Almacenamiento
-80°C, protect from light
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FZ-AD005 Related Classifications
HY-164729 Related Classifications
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