SGI-1776 free base

Catalog No.S2198

SGI-1776 free base Chemical Structure

Molecular Weight(MW): 405.42

SGI-1776 free base is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM in a cell-free assay, 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin. Phase 1.

Size Price Stock Quantity  
In DMSO USD 224 In stock
USD 140 In stock
USD 270 In stock
USD 670 In stock
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3 Customer Reviews

  • VCaP cells were steroid starved overnight then treated with 10nM R1881 and PIM kinase inhibitor SGI-1776 as indicated for 4 hours. Total protein lysates were analyzed by Western blot with antibodies against P-AR S213, AR (total), P-4EBP1 Thr 37/46, and tubulin.

    Oncogene 2013 32(34), 3992-4000. SGI-1776 free base purchased from Selleck.

    (A,B) PC3 or DU-145 cells were treated with suboptimal concentrations of Gefitinib, SGI-1776, M-110 or combinations of Gefitinib and SGI-1776 or M-110. Cell proliferation was measured after 72 hrs using the SRB assay.

    Oncotarget 2011 2(12), 1134-44. SGI-1776 free base purchased from Selleck.

  • Mean IL-8 concentrations determined by ELISA of the supernatants of HeLa cells infected with wild-type Salmonella. Kinase inhibitors are indicated on the x axis, and the target families of the inhibitors are indicated above each column. CEC, chelerythrine; Pim Inh, Pim-1 inhibitor 2. Inhibitors that significantly affected IL-8 production relative to the control (P < 0.05, Bonferroni post hoc test from one-way ANOVA) are indicated with an asterisk. Relative cell viability is also shown, as determined by reduction of XTT by viable cells. A450, absorbance at 450 nm.

    Sci Signal 2011 4, rs9. SGI-1776 free base purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description SGI-1776 free base is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM in a cell-free assay, 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin. Phase 1.
Targets
Pim1 [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
Pim3 [1]
(Cell-free assay)
Pim2 [1]
(Cell-free assay)
7 nM 44 nM 69 nM 363 nM
In vitro

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. [1]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. [2] 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. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO cells NVnjPVZETnWwY4Tpc44h[XO|YYm= M{[w[WlvcGmkaYTpc44hd2ZiaIXtZY4hTVKJIHX4dJJme3OnZDDpckBEUE9iY3XscJMh[nliYYX0c41ifGWmIIDheINpKGOuYX3wJI1mfGixZDygTWM2OD1zIN88US=> MmnrNlU2QDl7M{K=

... Click to View More Cell Line Experimental Data

In vivo Consistent with cell line data, xenograft model studies with mice bearing MV-4-11 tumors shows efficacy with SGI-1776. [1] SGI-1776 has shown preclinical activity against leukemia and solid tumor cell line models with IC50 values of 0.005–11.68 mM. SGI-1776 induces significant differences in EFS distribution in vivo in 9 of 31 solid tumor xenografts and in 1 of 8 of the evaluable ALL xenografts. [3]

Protocol

Kinase Assay:[2]
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Kinase Assays:

Kinase inhibition is measured by the use of radiometric assays performed by KinaseProfiler service. Assays contain a peptide substrate, known purified recombinant human kinases, gamma-labeled ATP, magnesium ion, and a fixed concentration (1 μM) of SGI-1776. In a final reaction volume of 25 μL, 5 to 10 mU of Pim1/2/3 is incubated with 8 mM of MOPS, pH 7.0; 0.2 mM ethylene diamine tetraacetic acid; 100 μM KKRNRTLTV;10 mM MgAcetate; and [γ-32P-ATP] . The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 5 μL of a 3% phosphoric acid solution. Then, 10 μL of the reaction is spotted onto a P30 filtermat and washed 3 times for 5 minutes in 75 mM phosphoric acid and once in methanol before it is dried and measured via a scintillation counter.
Cell Research:[1]
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  • Cell lines: MV-4-11, MOLM-13, and OCI-AML-3 cell lines
  • Concentrations: 0.1-10 μM
  • Incubation Time: 24 hours
  • Method: Cells are cultured in IMDM (ATCC) supplemented with 10% FBS and grown in a 37oC incubator with 5% CO2. Cells are routinely tested for Mycoplasma infection using a commercially available kit. Cells are treated with DMSO or various concentrations of SGI-1776 for 24 hours. Cells (1×106) are washed, then resuspended in 100 μL of annexin binding buffer, mixed with 5 μL of FITC solution and 5 μL of propidium iodide (PI; 50 μg/mL) solution. For each sample, 1×104 cells are measured using a Becton Dickinson FACSCalibur flow cytometer.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Female cNOD-SCID mice
  • Formulation: 5% dextrose
  • Dosages: 75 mg/kg and 200 mg/kg
  • Administration: Administered via oral gavage (PO) on a daily ×5/week or twice/week schedu
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 81 mg/mL (199.79 mM)
Ethanol 81 mg/mL (199.79 mM)
Water Insoluble
In vivo Add solvents individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 405.42
Formula

C20H22F3N5O

CAS No. 1025065-69-3
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01239108 Withdrawn Relapsed/Refractory Leukemias Astex Pharmaceuticals October 2010 Phase 1
NCT00848601 Terminated Prostate Cancer|Non-Hodgkins Lymphoma Astex Pharmaceuticals February 2009 Phase 1

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Pim Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID