2. Antibody-drug Conjugate/ADC Related Immunology/Inflammation Cell Cycle/DNA Damage Apoptosis
  3. Antibody-Drug Conjugates (ADCs) Mucin Topoisomerase Apoptosis
  4. DS-3939a

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 Exatecan (HY-13631). 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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DS-3939a

DS-3939a Chemical Structure

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DS-3939a Related Antibodies

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Description

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 Exatecan (HY-13631). 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[1].

IC50 & Target[1]

MUC1

 

Topoisomerase I

 

In Vitro

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.

DS-3939a Related Antibodies

Western Blot Analysis[1]

Cell Line: TA-MUC1-positive CFPAC-1 cells
Concentration: 3 μg/mL
Incubation Time: 2 d
Result: Upregulated the expression of γH2AX and cleaved PARP in TA-MUC1-positive CFPAC-1 cells.
In Vivo

DS-3939a (0.25-8 mg/kg, i.v., once on day 0) exhibits dose-dependent tumor growth inhibition in female nude mice bearing CFPAC-1 pancreatic cancer xenografts [1].
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.

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]
Dosage: 0.25, 0.5, 1, 2, 4, 8 mg/kg
Administration: i.v., once on day 0
Result: Achieved dose-dependent tumor growth inhibition.
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]
Dosage: 10 mg/kg
Administration: i.v., once on day 0
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.
SMILES

[DS-3939a]
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DS-3939a Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

DS-3939aDS-3939DS3939DS 3939Antibody-Drug Conjugates (ADCs)MucinTopoisomeraseApoptosisAntibody-Drug Conjugatesantibody-drug conjugateMUC1cancersapoptosisInhibitorinhibitorinhibit

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