STF-083010

Catalog No.S7771

For research use only.

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

STF-083010 Chemical Structure

CAS No. 307543-71-1

Selleck's STF-083010 has been cited by 22 publications

Purity & Quality Control

Choose Selective IRE1 Inhibitors

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SF21 cell NYPTUY9TTnWwY4Tpc44h[XO|YYm= M1W3WmlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRicIXybZRqdi2KaYOteIFo\2WmIFnSSU0yKFKQYYPlJIV5eHKnc4Pl[EBqdiCVRkKxJINmdGy|IIXzbY5oKFiEUD2xJHJPSSC|dHXtJIxwd3BiYYOgd5Vje3S{YYTlJIlv[3WkYYTl[EBnd3JiM{CgcYlveyCycnnvdkB1dyC|dXLzeJJifGViYXTkbZRqd25ibXXhd5Vz\WRiYX\0[ZIhOiCqcoOgZpkhTlKHVD3zeZBxemW|c3nvckBie3OjeTygTWM2OD17LkmzPUDPxE1? M4i2[|I1PzR7OE[x
Assay
Methods Test Index PMID
Growth inhibition assay Cell count 29423023
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 Research:[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 Research:[1]
  • Animal Models: NOD/SCID/IL2Rγ null mice
  • Dosages: 30 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+40%PEG 300+5% Tween80 +ddH2O
For best results, use promptly after mixing.

2mg/mL

Chemical Information

Molecular Weight 317.38
Formula

C15H11NO3S2

CAS No. 307543-71-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C2C(=C1)C=CC(=C2C=NS(=O)(=O)C3=CC=CS3)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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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
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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.

Molarity Calculator

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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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