DS-3939a
Based on 1 Customer Validation
DS-3939a (DS-3939) is an anti-TA-MUC1 (tumor-associated mucin-1) antibody-drug conjugate (ADC). DS-3939a consists of a humanized anti-TA-MUC1 IgG1 monoclonal antibody Gatipotuzumab ( HY-P99634), a stable and cleavable tetrapeptide-based linker (Gly-Gly-Phe-Gly), and a DNA topoisomerase I inhibitor payload (DXd) (HY-13631D), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E). DS-3939a inhibits the growth of TA-MUC1-positive cancer cells (CFPAC-1, NCI-H2110) by inducing DNA damage and apoptosis. DS-3939a exhibits significant antitumor activity in a variety of TA-MUC1-expressing advanced solid tumors. DS-3939a can be used for the study of TA-MUC1-expressing advanced cancers.
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-80°C, protect from light
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Actividad biológica
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Actividad biológica
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MUC1 |
Topoisomerase I |
DS-3939a (0.01-10000 ng/mL, 6 d) inhibits the growth of TA-MUC1-positive CFPAC-1 and NCI-H2110 cells[1].
DS-3939a (3 μg/mL, 2 d) upregulates the expression of γH2AX and cleaved PARP in TA-MUC1-positive CFPAC-1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:TA-MUC1-positive CFPAC-1 cells
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Concentration:3 μg/mL
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Incubation Time:2 d
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Result:Upregulated the expression of γH2AX and cleaved PARP in TA-MUC1-positive CFPAC-1 cells.
DS-3939a (10 mg/kg, i.v., once on day 0) exerts potent antitumor activity against TA-MUC1-positive NCI-H2110 lung cancer xenografts but no effect on TA-MUC1-negative HCT-15 colorectal cancer xenografts in female nude mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CFPAC-1 pancreatic cancer cells (1.0×107 cells in 0.1 mL saline) were subcutaneously implanted into the right flanks of 4-5-week-old female nude mice[1]
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Dosage:0.25, 0.5, 1, 2, 4, 8 mg/kg
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Administration:i.v., once on day 0
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Result:Achieved dose-dependent tumor growth inhibition.
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Animal Model:NCI-H2110 lung cancer cells or HCC70 triple-negative breast cancer cells were subcutaneously implanted into the flanks of 4-5-week-old female nude mice[1]
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Dosage:10 mg/kg
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Administration:i.v., once on day 0
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Result:Exerted potent antitumor activity against TA-MUC1-positive NCI-H2110 lung cancer xenografts but no effect on TA-MUC1-negative HCT-15 colorectal cancer xenografts.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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Appearance Liquid
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Color Colorless to light yellow
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SMILES
[DS-3939a]
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Synonyms
DS-3939
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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 (273 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)
DS-3939a Related Classifications
HY-177442 Related Classifications
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