STF083010 是一种 IRE1α 核酸内切酶的选择性抑制剂。

STF-083010 is a selective inhibitor of the IRE1α endonuclease.

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.

STF-083010 (i.p., 30 mg/kg) signi?cantly inhibits the growth of the tumor in human multiple myeloma (MM) xenografts model.

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.

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.

NOD/SCID/IL2Rγ null mice were injected intraperitoneally of STF-083010(30 mg/kg) dissolved in 16% chremophor.

307543-71-1

C15H11NO3S2

317.38

STF083010

DMSO:31.7 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years