Home Tools

SGI-1776

Catalog No. T3078 CAS 1025065-69-3

Synonyms: SGI-1776 free base, Pim-Kinase Inhibitor IX

SGI-1776 (Pim-Kinase Inhibitor IX) has been used in trials studying the treatment of Prostate Cancer, Non-Hodgkins Lymphoma, and Relapsed/Refractory Leukemias.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

SGI-1776, CAS 1025065-69-3

Pack Size	Availability	Price/USD
2 mg	In stock	$ 48.00
5 mg	In stock	$ 98.00
10 mg	In stock	$ 175.00
25 mg	In stock	$ 320.00
50 mg	In stock	$ 461.00
100 mg	In stock	$ 591.00
1 mL * 10 mM (in DMSO)	In stock	$ 100.00

Bulk Inquiry

Select Batch

Purity: 100%

Purity: 99.84%

Purity: 99.3%

Purity: 99.03%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	SGI-1776 (Pim-Kinase Inhibitor IX) has been used in trials studying the treatment of Prostate Cancer, Non-Hodgkins Lymphoma, and Relapsed/Refractory Leukemias.
Targets&IC50	FLT3:44 nM, Pim1:7 nM, Pim3:69 nM, Pim2:363 nM
In vitro	SGI-1776 has demonstrated preclinical activity against leukemia and solid tumor cell line models, with IC50 values ranging from 0.005 to 11.68 mM. It induced a significant difference in the distribution of in vivo EFS (event-free survival) in 9 out of 31 solid tumor xenografts and in 1 out of 8 evaluable ALL (acute lymphoblastic leukemia) xenografts. Furthermore, SGI-1776 has proven effective in mouse models harboring the MV-4-11 tumor.
In vivo	SGI-1776 induces dose-dependent apoptosis in CLL cells through a mechanism that involves a decrease in Mcl-1. Additionally, in vitro, SGI-1776 demonstrates cytotoxicity with an average relative IC50 value of 3.1 mM. Beyond targeting Pim, SGI-1776 effectively targets FLT3 with an IC50 of 44 nM. It also induces apoptosis in AML cells in a concentration-dependent manner and shows cytotoxic effects on primary AML cells, leading to a reduction in Mcl-1 protein.
Kinase Assay	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	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)

Synonyms	SGI-1776 free base, Pim-Kinase Inhibitor IX
Molecular Weight	405.42
Formula	C20H22F3N5O
CAS No.	1025065-69-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 75 mg/mL (185 mM)

Ethanol: 75 mg/mL (185 mM)

References and Literature

1. Chen LS, et al. Blood, 2011, 118(3), 693-702. 2. Chen LS, et al. Blood, 2009, 114(19), 4150-7. 3. Batra V, et al. Pediatr Blood Cancer, 2012, 59(4), 749-752.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Inhibitor Library Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Cancer Drug Library Anti-Pancreatic Cancer Compound Library NO PAINS Compound Library Anti-Lung Cancer Compound Library

Related Products

Related compounds with same targets

Physalin B (S)-(+)-Rolipram Sodium diatrizoate Oleic acid DB1976 Resveratrol Diallyl Trisulfide Quisinostat

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

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

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 n 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.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

SGI-1776 1025065-69-3 Angiogenesis Apoptosis Autophagy Chromatin/Epigenetic JAK/STAT signaling Tyrosine Kinase/Adaptors Pim FLT Inhibitor SGI 1776 Pim kinases SGI-1776 free base SGI1776 inhibit Pim-Kinase Inhibitor IX inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.