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SGI-1776

SGI-1776
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Purity:100%
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SGI-1776

Catalog No. T3078Cas No. 1025065-69-3
SGI-1776 (Pim-Kinase Inhibitor IX) has been used in trials studying the treatment of Prostate Cancer, Non-Hodgkins Lymphoma, and Relapsed/Refractory Leukemias.
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Pack SizePrice/USDAvailabilityQuantity
2 mg$48In Stock
5 mg$98In Stock
10 mg$175In Stock
25 mg$320In Stock
50 mg$461In Stock
100 mg$591In Stock
1 mL x 10 mM (in DMSO)$100In Stock
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Product Introduction

Bioactivity
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.
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)
AliasSGI-1776 free base, Pim-Kinase Inhibitor IX
Chemical Properties
Molecular Weight405.42
FormulaC20H22F3N5O
Cas No.1025065-69-3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 55.55 mg/ml (137.03 mM)
Ethanol: 75 mg/mL (185 mM)
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.4666 mL12.3329 mL24.6658 mL123.3289 mL
5 mM0.4933 mL2.4666 mL4.9332 mL24.6658 mL
10 mM0.2467 mL1.2333 mL2.4666 mL12.3329 mL
20 mM0.1233 mL0.6166 mL1.2333 mL6.1664 mL
50 mM0.0493 mL0.2467 mL0.4933 mL2.4666 mL
100 mM0.0247 mL0.1233 mL0.2467 mL1.2333 mL

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