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STF-083010 is a selective inhibitor of the IRE1α endonuclease.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $47 | In Stock | |
10 mg | $73 | In Stock | |
25 mg | $123 | In Stock | |
50 mg | $215 | In Stock | |
100 mg | $387 | In Stock | |
200 mg | $585 | In Stock | |
500 mg | $853 | In Stock | |
1 mL x 10 mM (in DMSO) | $53 | In Stock |
Description | STF-083010 is a selective inhibitor of the IRE1α endonuclease. |
In vitro | WaC3 cells respond to treatments with STF-083010 with gradually decreased growth. In MEC1 and MEC2 cells, STF-083010 produces 20% growth inhibition in 48 hours cultures. In MM.1R MM, MM.1S, and RPMI 8226 cell lines, STF-083010 displays cytostatic and cytotoxic activity in a dose and time-dependent manner. In Eμ-TCL1 CLL cells, STF-083010 displays about 70% growth inhibition after 3 days culture. In SU8686, Panc0403, and MiaPaCa2 cell lines, STF-083010 blocks IRE1α's endonuclease and inhibits XBP1 splicing activity without affecting its kinase activity. |
In vivo | STF-083010 (i.p., 30 mg/kg) signi?cantly inhibits the growth of the tumor in human multiple myeloma (MM) xenografts model. |
Kinase Assay | Autophosphorylation activity is measured by adding of 32P-γ ATP. Endonuclease activity is measured by the adding of radiolabeled HAC1 508-nt RNA substrate synthesized in vitro using α32P-UTP. Mix STF083010 with recombinant hIRE1 protein, radiolabeled HAC1 508 nt RNA, and appropriate buffers to incubate. Kinase activity is quantitated by polyacrylamide gel electrophoresis. RNAsecleavage products are quantitated by 32P-γATP or 32P-UTP autoradiography. |
Cell Research | 3×10E3 (Panc0403, Panc1005, BxPc3, and MiaPaCa2) cell lines are seeded in 96-well plates overnight, and STF-083010(~50 μM) treatment for 48 hours started the next day. |
Animal Research | NOD/SCID/IL2Rγ null mice were injected intraperitoneally of STF-083010(30 mg/kg) dissolved in 16% chremophor. |
Alias | STF083010 |
Molecular Weight | 317.38 |
Formula | C15H11NO3S2 |
Cas No. | 307543-71-1 |
Smiles | O=C1C=Cc2ccccc2\C1=C\NS(=O)(=O)c1cccs1 |
Relative Density. | 1.40 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 40 mg/mL (126.03 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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