伊斯平斯

溶解度:Unknown

储存条件:at -20℃ 2 years

生物活性

SGI-1776, a member of the imidazo[1,2-b]pyridazine chemical class, was selected for its ability to exploit an extended ATP-binding and solvent pocket, thereby making it a selective Pim family kinase inhibitor.Extensive biochemical characterization of SGI-1776 confirmed its specificity for the three isoforms of the Pim family.The IC₅₀ of SGI-1776 for the three isoforms of the Pim kinase family, Pim-1, Pim-2, and Pim-3, were in the low nanomolar range (7 ± 1.8 nmol/L, 363 ± 27.6 nmol/L, and 69 ± 9.2 nmol/L).SGI-1776 is a fairly selective inhibitor of the Pim kinases and can cause a reduction in prostate cancer cell viability and alter overall cytotoxic responses to taxanes. SGI-1776 can disrupt cell cycle progression, induce apoptosis, promote taxane sensitivity, and overcome acquired chemoresistance by inhibiting multidrug resistance (MDR)1 activity in specific prostate cancer models.SGI-1776 induces apoptosis in CLL and that the mechanism involves Mcl-1 reduction.SGI-1776 exhibited inhibitory activity against two other kinases: Flt-3 (IC₅₀, 44 nmol/L) and Haspin (IC₅₀, 34 nmol/L).

参考文献

[1] Mumenthaler, S. M., P. Y. Ng, et al. (2009).Mol Cancer Ther 8(10): 2882-2893.