SGI-1776

SKU: orb1304563

Description

SGI-1776 is a Pim kinase inhibitor investigated in preclinical and clinical research for hematological and solid tumors. Studies have explored its application in prostate cancer, non-Hodgkin's lymphoma, and relapsed/refractory leukemias, demonstrating activity in both in vitro and in vivo models.

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 1025065-69-3
• MW: 405.42
• Purity: >99.99% (May vary between batches)
• Formula: C₂₀H₂₂F₃N₅O
• SMILES: CN1CCC(CNc2ccc3ncc(-c4cccc(OC(F)(F)F)c4)n3n2)CC1
• Target: Apoptosis,Autophagy,FLT,Pim
• Solubility: Ethanol:75 mg/mL (184.99 mM);10% DMSO+40% PEG300+5% Tween-80+45% Saline:2.5 mg/mL (6.17 mM);DMSO:52 mg/mL (128.26 mM)

Bioactivity

• Target IC50:
  Pim3:69 nM|Pim2:363 nM|FLT3:44 nM|Pim1:7 nM
• 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.
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• 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.
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• 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)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Pim, Pim1, Pim3, Pim2, Pim-Kinase Inhibitor IX, SGI 1776, SGI1776, SGI-1776, SGI-1776 free base, Autophagy, Apoptosis, FLT3

Compound Identifiers

PubChem CID

24795070