Subasumstat (TAK-981)

Catalog No.S8829

For research use only.

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

Subasumstat (TAK-981) Chemical Structure

CAS No. 1858276-04-6

Selleck's Subasumstat (TAK-981) has been cited by 2 Publications

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 (from reference)

Cell Research:

[1]

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

    --

Animal Research:

[2]

  • Animal Models: immune-competent BALB/c mice
  • Dosages: 7.5 mg/kg
  • Administration: IV

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 578.10
Formula

C25H28ClN5O5S2

CAS No. 1858276-04-6
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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

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