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STF-083010 IRE1 inhibitor

Name: STF-083010
SKU: S7771
Availability: InStock
Rating: 5 (38 reviews)

Cat.No.S7771

STF-083010 is a specific IRE1α endonuclease inhibitor without affecting its kinase activity.

Chemical Structure

Molecular Weight: 317.38

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.08%

99.08

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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
SF21 cell	Function assay				Inhibition of human recombinant puritin-His-tagged IRE-1 RNase expressed in SF21 cells using XBP-1 RNA stem loop as substrate incubated for 30 mins prior to substrate addition measured after 2 hrs by FRET-suppression assay, IC50=9.939 μM
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	317.38	Formula	C₁₅H₁₁NO₃S₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	307543-71-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC=C2C(=C1)C=CC(=C2C=NS(=O)(=O)C3=CC=CS3)O

Solubility

In vitro
Batch:

DMSO : 63 mg/mL (198.5 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.	1.000mg/ml (3.15mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 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.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.350mg/ml (1.10mM)	Taking the 1 mL working solution as an example, add 50 μL of 7 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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	IRE1α endonuclease ^[1]
In vitro	In RPMI 8226, MM.1S, and MM.1R MM cell lines, STF-083010 exhibits cytostatic and cytotoxic activity in a dose and time dependent manner. ^[1] ^[2] In MiaPaCa2, Panc0403, and SU8686 cell lines, this compound inhibits XBP1 splicing and blocks IRE1α's endonuclease activity without affecting its kinase activity. ^[1] In Eμ-TCL1 CLL cells, it exhibits about 70% growth inhibition after 3 days culture. In MEC1 and MEC2 cells, this chemical produces 20% growth inhibition in 48 h. WaC3 cells respond to treatments with this compound with gradually decreased growth. ^[3]
Kinase Assay	Cell free IRE1 assays
Kinase Assay	Autophosphorylation activity is determined by the addition of ³²P-γ ATP. Endonuclease activity is determined by the addition of radiolabeled HAC1 508-nt RNA substrate synthesized in vitro using α³²P-UTP. STF083010 is incubated with recombinant hIRE1 protein, radiolabeled HAC1 508 nt RNA, and appropriate buffers. Kinase activity is quantitated by polyacrylamide gel electrophoresis. RNAsecleavage products are quantitated by ³²P-γATP or ³²P-UTP autoradiography.
In vivo	In human multiple myeloma (MM) xenografts model, STF-083010 (i.p., 30 mg/kg) signiﬁcantly inhibits the growth of tumor. ^[1]
References	[1] https://pubmed.ncbi.nlm.nih.gov/21081713/ [2] https://pubmed.ncbi.nlm.nih.gov/24952679/ [3] https://pubmed.ncbi.nlm.nih.gov/22692508/

Applications

Methods	Biomarkers	Images	PMID
Growth inhibition assay	Cell count		29423023

Tech Support

Handling Instructions

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