SGI-1776 free base

For research use only.

Catalog No.S2198

16 publications

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  
10mM (1mL in DMSO) USD 224 In stock
USD 140 In stock
USD 270 In stock
USD 670 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's SGI-1776 free base has been cited by 16 publications

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.

  • 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.

  • (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.

Purity & Quality Control

Choose Selective Pim Inhibitors

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.
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 M4nWO2Z2dmO2aX;uJIF{e2G7 M4juNGlvcGmkaYTpc44hd2ZiaIXtZY4hTVKJIHX4dJJme3OnZDDpckBEUE9iY3XscJMh[nliYYX0c41ifGWmIIDheINpKGOuYX3wJI1mfGixZDygTWM2OD1zIN88US=> MXmyOVU5QTl|Mh?=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
c-Myc (Ser62) / c-Myc / p-Histone H3 (Ser10) / Histone H3 / Bad(Ser112) / Bad / 4E-BP1 ; 

PubMed: 22955922     

Effect of SGI-1776 on phospho-c-Myc (Ser62) and total c-Myc (A) phospho-Histone H3 (Ser10) and total Histone H3 (B), phospho-Bad (Ser112) and total Bad (C), and phospho-4E-BP1(Thr37/46) and total 4E-BP1 (D) protein expressions. JeKo-1 and Mino cell were treated with 0.1, 1, 3, 5, or 10μM SGI-1776 for 24 hours, and then cell lysates were analyzed via immunoblot. 


PubMed: 22955922     

Impact of SGI-1776 in dose-dependent (E) treatments on Mcl-1 protein expression in JeKo-1 and Mino cells. Mcl-1 protein expression was measured by immunoblots.

Cell viability ; 

PubMed: 22015557     

SGI-1776 reduces RCC cell viability. Five RCC cell lines and RPTEC cells were incubated with the indicated concentrations of SGI-1776 for 72 h and cell viability was measured by MTT assay. Mean±s.d., n=3.

p70-S6K / p-P70S6K / rpS6 / p-rpS6 ; 

PubMed: 27120806     

LN229 cells were treated with SGI-1776 (5 μM) for the indicated times. Equal amounts of total cell lysates were subjected to SDS-PAGE followed by immunoblotting with antibodies against the phosphorylated forms of p70-S6K (pThr389), rpS6 (pSer235/236), or against HSP90 as indicated. Equal amounts of cell lysates from the same experiment were analyzed in parallel by SDS-PAGE and immunoblotted with antibodies against p70-S6K or rpS6, as indicated. 

22955922 22015557 27120806
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]


Kinase Assay:[2]
- Collapse

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]
- Collapse
  • 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]
- Collapse
  • Animal Models: Female cNOD-SCID mice
  • 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 to the product individually and in order(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.
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


CAS No. 1025065-69-3
Storage powder
in solvent
Synonyms N/A
Smiles CN1CCC(CC1)CNC2=N[N]3C(=NC=C3C4=CC=CC(=C4)OC(F)(F)F)C=C2

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Pim Signaling Pathway Map

Related Pim Products

Tags: buy SGI-1776 free base | SGI-1776 free base supplier | purchase SGI-1776 free base | SGI-1776 free base cost | SGI-1776 free base manufacturer | order SGI-1776 free base | SGI-1776 free base distributor
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID