SGI-1776 free base is a selective Pim family kinase inhibitor with IC50 of 7 ¡À 1.8, 363 ¡À 27.6 and 69 ¡À 9.2 nM for Pim-1, Pim-2, and Pim-3, respectively. SGI-1776 is 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. 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 MDR1 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 nM) and Haspin (IC50= 34 nM).

June 21, 2017

prudect name : SGI-1776 free base is a selective Pim family kinase inhibitor with IC50 of 7 ¡À 1.8, 363 ¡À 27.6 and 69 ¡À 9.2 nM for Pim-1, Pim-2, and Pim-3, respectively.
SGI-1776 is 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. 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 MDR1 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 nM) and Haspin (IC50= 34 nM).
SGI-1776

Synonyms: CAS NO: 1025065-69-3 Molecular Formula: C₂₀H₂₂F₃N₅OMolecular Weight: 405.42Purity: 98% minSolubility: In DMSOStorage: -20°C

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