FZ-AD005
Based on 1 Customer Validation
FZ-AD005 is an antibody-drug conjugate (ADC) that selectively targets DLL3, generated by conjugating the anti-DLL3 antibody FZ-A038 (HY-P990896) with a dipeptide linker (Val-Ala) and DXd (HY-13631D). FZ-AD005 binds human DLL3 with a Kd of 58.3 pM. FZ-AD005 binds cell-surface DLL3 and mediates internalization, followed by lysosomal cathepsin cleavage to release the payload DXd, which induces DNA double-strand breaks, cell cycle arrest, and apoptosis through inhibition of topoisomerase TopI, and exhibits a bystander killing effect on adjacent DLL3-negative cells. FZ-AD005 can be used for research on small cell lung cancer and human neuroendocrine prostate cancer.
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- Pureté : 97.04%
- Masse moléculaire:154128 (average)
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Stockage:Shipping with dry ice
-80°C, protect from light
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Activité biologique
Description
IC50 & Target
[1]|
Topoisomerase I |
DLL3 58.3 pM (Kd) |
In Vitro
FZ-AD005 (100 μg/mL; 7 d) is highly stable in human plasma, releasing only about 0.7% of DXd[1] after 7 days of incubation at 37℃.
FZ-AD005 (200 pmol; 48 h) rapidly internalizes into DLL3-expressing cells within 30 minutes, traffics to lysosomes, and releases DXd in a time-dependent manner over the 48-hour test period[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 h
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Result:Effectively eliminated both NCI-H82 and Ramos cell populations in the coculture system.
Parmacokinetics
In Vivo
FZ-AD005 (1.5-6 mg/kg; i.v.; 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; i.v.; 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; i.v.; 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.\n
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.\n
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.\n
Demonstrated notably superior efficacy to lurbinectedin (23.48% TGI at 0.18 mg/kg).\n
Caused no obvious body weight loss in treated mice.
Chemical Information
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Appearance Liquid
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Masse moléculaire 154128 (average)
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Color Colorless to light yellow
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SMILES
[FZ-AD005]
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Livraison
Shipping with dry ice.
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Stockage
-80°C, protect from light
Pureté et documentation
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Fiche technique (283 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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Instruction de manipulation (2659 KB)
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FZ-AD005 Related Classifications
HY-164729 Related Classifications
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