STF-083010

Catalog No.S7771 Batch:S777103

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Technical Data

Formula

C15H11NO3S2
Molecular Weight 317.38 CAS No. 307543-71-1
Solubility (25°C)* In vitro DMSO 63 mg/mL (198.5 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.35mg/ml 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. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.0mg/ml 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. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description STF-083010 is a specific IRE1α endonuclease inhibitor without affecting its kinase activity.
Targets
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, STF-083010 inhibits XBP1 splicing and blocks IRE1α's endonuclease activity without affecting its kinase activity. [1] In Eμ-TCL1 CLL cells, STF-083010 exhibits about 70% growth inhibition after 3 days culture. In MEC1 and MEC2 cells, STF-083010 produces 20% growth inhibition in 48 h. WaC3 cells respond to treatments with STF-083010 with gradually decreased growth. [3]
In vivo In human multiple myeloma (MM) xenografts model, STF-083010 (i.p., 30 mg/kg) significantly inhibits the growth of tumor. [1]

Protocol (from reference)

Kinase Assay:[1]
  • Cell free IRE1 assays

    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.
Cell Assay:[1]
  • Cell lines

    Panc0403, Panc1005, BxPc3, and MiaPaCa2 cell lines

  • Concentrations

    ~50 μM

  • Incubation Time

    ~48 h

  • Method

    Three thousand cells are seeded in 96-well plates overnight and drug treatment started the next day. After 48 h incubation, MTT is added to cells and cultured at 37℃ for 4 h followed by stop solution (4 mM HCl, 0.1% Nondet P40 in isopropanol) which is added to dissolve MTT. The plates are read with a spectrophotometer at 590 nm absorbance with reference at 630 nm. IC50 values are calculated using GraphPad Prism.
Animal Study:[1]
  • Animal Models

    NOD/SCID/IL2Rγ null mice

  • Dosages

    30 mg/kg

  • Administration

    i.p.

Customer Product Validation

, , Mol Cell Endocrinol, 2016, 434:48-56.

Data from [Data independently produced by , , Front Mol Neurosci, 2018, 11:72]

Data from [Data independently produced by , , Neurochem Res, 2018, 43(3):669-680]

Selleck's STF-083010 has been cited by 35 publications

Palmitate induces integrated stress response and lipoapoptosis in trophoblasts [ Cell Death Dis, 2024, 15(1):31] PubMed: 38212315
HRS mediates tumor immune evasion by regulating proteostasis-associated interferon pathway activation [ Cell Rep, 2023, 10.1016/j.celrep.2023.113352] PubMed: 37948180
Acute Endoplasmic Reticulum Stress Suppresses Hepatic Gluconeogenesis by Stimulating MAPK Phosphatase 3 Degradation [ Int J Mol Sci, 2023, 24(21)15561] PubMed: 37958545
Emodin, an Emerging Mycotoxin, Induces Endoplasmic Reticulum Stress-Related Hepatotoxicity through IRE1α-XBP1 Axis in HepG2 Cells [ Toxins (Basel), 2023, 15(7)455] PubMed: 37505724
Emodin, an Emerging Mycotoxin, Induces Endoplasmic Reticulum Stress-Related Hepatotoxicity through IRE1α-XBP1 Axis in HepG2 Cells [ Toxins (Basel), 2023, 15(7)455] PubMed: 37505724
IRE1α/XBP-1 promotes β-catenin signaling activation of airway epithelium in lipopolysaccharide-induced acute lung injury [ Pulm Pharmacol Ther, 2023, 10.1016/j.pupt.2023.102263] PubMed: 37935327
UPF3B modulates endoplasmic reticulum stress through interaction with inositol-requiring enzyme-1α [ Research Square, 2023, ] PubMed: none
Scleral PERK and ATF6 as targets of myopic axial elongation of mouse eyes [ Nat Commun, 2022, 13(1):5859] PubMed: 36216837
Pharmacologic IRE1/XBP1s activation promotes systemic adaptive remodeling in obesity [ Nat Commun, 2022, 13(1):608] PubMed: 35105890
Tp47 promoted the phagocytosis of HMC3 cells though autophagy induced by endoplamic reticlum stress [ J Eur Acad Dermatol Venereol, 2022, 10.1111/jdv.18295] PubMed: 35666816

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.