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).

By VD/VDR- vd-vdr 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

web site: www.medchemexpress.com

In addition to Pim, SGI-1776 also potently targets FLT3 (IC50 = 44nM). Treatment of AML cells with SGI-1776 results in a concentration-dependent induction of apoptosis. Importantly, SGI-1776 is also cytotoxic in AML primary cells, irrespective of FLT3 mutation status and results in Mcl-1 protein decline.Treatment of CLL cells with SGI-1776 results in a concentration-dependent induction of apoptosis. SGI-1776 induces apoptosis in CLL and that the mechanism involves Mcl-1 reduction. Apoptosis induction coupled with the inhibition of RNA synthesis is observed in CLL cells treated with SGI-1776. SGI-1776 exhibites cytotoxic activity in vitro with a median relative IC50 of 3.1 mM. SGI-1776 induces tumor growth inhibition meeting criteria for intermediate EFS T/C activity in 1 of 39 evaluable models. In contrast, SGI-1776 induces complete responses of subcutaneous MV4;11.

By VD/VDR- vd-vdr June 21, 2017

prudect name : In addition to Pim, SGI-1776 also potently targets FLT3 (IC50 = 44nM). Treatment of AML cells with SGI-1776 results in a concentration-dependent induction of apoptosis. Importantly, SGI-1776 is also cytotoxic in AML primary cells, irrespective of FLT3 mutation status and results in Mcl-1 protein decline.Treatment of CLL cells with SGI-1776 results in a concentration-dependent induction of apoptosis. SGI-1776 induces apoptosis in CLL and that the mechanism involves Mcl-1 reduction. Apoptosis induction coupled with the inhibition of RNA synthesis is observed in CLL cells treated with SGI-1776. SGI-1776 exhibites cytotoxic activity in vitro with a median relative IC50 of 3.1 mM. SGI-1776 induces tumor growth inhibition meeting criteria for intermediate EFS T/C activity in 1 of 39 evaluable models. In contrast, SGI-1776 induces complete responses of subcutaneous MV4;11.
SGI-1776

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

web site: www.medchemexpress.com

By VD/VDR- vd-vdr

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