Name: Subasumstat (TAK-981)
Brand: Selleck Chemicals
SKU: S8829
Rating: 5 (17 reviews)

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Quality Control

Batch: Purity: 99.57%

99.57

Related Targets	Proteasome E1 Activating E3 Ligase DUB p97 E2 conjugating
Other SUMO Inhibitors	2-D08 Ginkgolic Acid momordin-Ic Ginkgolic Acid (C13:0)

Chemical Information, Storage & Stability

Molecular Weight	578.10	Formula	C₂₅H₂₈ClN₅O₅S₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1858276-04-6	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin 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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (172.98 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (8.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Mechanism of Action

Targets/IC₅₀/Ki	SUMOylation enzymatic cascade
In vitro	Ex vivo treatment with Subasumstat (TAK-981) induced markers of activation and maturation—including CD40, CD80, and CD86—as well as increased secretion of inflammatory cytokines such as IP-10, MCP1, MIP-1α, MIP1β, IFNα, and IFNβ, in both mouse bone-marrow and human peripheral blood mononuclear cell derived dendritic cells (DCs).
In vivo	In vivo, a single sub-cutaneous injection of Subasumstat (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. This compound demonstrates antitumor activity, including complete regression (CR) of some tumours, in immune-competent BALB/c mice bearing syngeneic A20 lymphoma tumours.
References	[1] https://cancerres.aacrjournals.org/content/79/13_Supplement/3252.short [2] https://cancerres.aacrjournals.org/content/79/13_Supplement/3079.short

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04381650	Active not recruiting	Advanced or Metastatic Solid Tumors	Takeda\|Takeda Development Center Americas Inc.	August 17 2020	Phase 1\|Phase 2
NCT04074330	Terminated	Lymphoma Non-Hodgkin	Takeda	October 15 2019	Phase 1\|Phase 2
NCT03648372	Terminated	Neoplasms\|Lymphoma\|Hematologic Neoplasms	Takeda	October 1 2018	Phase 1\|Phase 2

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Handling Instructions

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Subasumstat (TAK-981) SUMOylation Inhibitor

Chemical Structure

Molecular Weight: 578.10