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

在化学研究中，WaC3细胞经STF-083010处理后显示出逐渐下降的生长率。在MEC1和MEC2细胞中，STF-083010在48小时培养中产生20%的生长抑制。在MM.1R MM、MM.1S及RPMI 8226细胞系中，STF-083010以剂量和时间依赖的方式展现了细胞静止和细胞毒性活性。在Eμ-TCL1 CLL细胞中，经过3天的培养，STF-083010显示出约70%的生长抑制。在SU8686、Panc0403和MiaPaCa2细胞系中，STF-083010阻断IRE1α的内切酶活性，并抑制XBP1剪接活性，而不影响其激酶活性。

STF-083010（i.p.，30 mg/kg）在人类多发性骨髓瘤（MM）异种移植模型中显著抑制了肿瘤的生长。

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.