Subasumstat (TAK-981)

For research use only.

Catalog No.S8829

Subasumstat (TAK-981) Chemical Structure

CAS No. 1858276-04-6

Subasumstat (TAK-981) is a novel, selective inhibitor of the SUMOylation enzymatic cascade with potential immune-activating and antineoplastic activities.

Purity & Quality Control

Choose Selective SUMO Inhibitors

Biological Activity

Description Subasumstat (TAK-981) is a novel, selective inhibitor of the SUMOylation enzymatic cascade with potential immune-activating and antineoplastic activities.
Targets
SUMOylation enzymatic cascade [1]
()
In vitro

In both mouse bone-marrow and human peripheral blood mononuclear cell derived dendritic cells (DCs), TAK-981 treatment ex vivo induced markers of activation and maturation including CD40, CD80 and CD86, as well as increased secretion of inflammatory cytokines like IP-10, MCP1, MIP-1α, MIP1β, IFNα and IFNβ.[1]

In vivo

In vivo, a single sub-cutaneous injection of TAK-981 in naïve Balb/c mice at the brachial lymph nodes induced activation of DCs, measured as significant increases in CD40 and CD86 expression.[1] TAK-981 demonstrates antitumor activity, including complete regression (CR) of some tumors, in immune-competent BALB/c mice bearing syngeneic A20 lymphoma tumors.[2]

Protocol

Cell Research:

[1]

- Collapse
  • Cell lines: mouse bone-marrow and human peripheral blood mononuclear cell derived dendritic cells (DCs)
  • Concentrations: --
  • Incubation Time: --
  • Method:

    --


    (Only for Reference)
Animal Research:

[2]

- Collapse
  • Animal Models: immune-competent BALB/c mice
  • Dosages: 7.5 mg/kg
  • Administration: IV
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (172.98 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 578.10
Formula

C25H28ClN5O5S2

CAS No. 1858276-04-6
Storage powder
in solvent
Synonyms N/A
Smiles CC1=C(C=C(S1)C(=O)C2=CN=CN=C2NC3CC(C(C3)O)COS(=O)(=O)N)C4C5=C(CCN4)C=CC(=C5)Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04381650 Recruiting Drug: TAK-981|Drug: Pembrolizumab Advanced or Metastatic Solid Tumors Takeda|Takeda Development Center Americas Inc. August 17 2020 Phase 1|Phase 2
NCT04074330 Recruiting Drug: TAK-981|Drug: Rituximab Lymphoma Non-Hodgkin Takeda October 15 2019 Phase 1|Phase 2
NCT03648372 Recruiting Drug: TAK-981 Neoplasms|Lymphoma|Hematologic Neoplasms Takeda October 1 2018 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field
Tags: buy Subasumstat (TAK-981) | Subasumstat (TAK-981) supplier | purchase Subasumstat (TAK-981) | Subasumstat (TAK-981) cost | Subasumstat (TAK-981) manufacturer | order Subasumstat (TAK-981) | Subasumstat (TAK-981) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID