1. JAK/STAT Signaling
    Stem Cell/Wnt
    PROTAC
  2. STAT
    Ligand for Target Protein for PROTAC
  3. SI-109

SI-109 

Cat. No.: HY-129603 Purity: 99.48% ee.: 99.67%
Handling Instructions

SI-109 is a potent STAT3 SH2 domain inhibitor (Ki=9 nM) with antitumor activity. SI-109 effectively inhibits the transcriptional activity of STAT3 (IC50=3 μM). SI-109 and an analog of CRBN ligand lenalidomide have been used to design PROTAC STAT3 degrader SD-36.

For research use only. We do not sell to patients.

SI-109 Chemical Structure

SI-109 Chemical Structure

CAS No. : 2429877-30-3

Size Price Stock Quantity
5 mg USD 2200 In-stock
Estimated Time of Arrival: December 31
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Description

SI-109 is a potent STAT3 SH2 domain inhibitor (Ki=9 nM) with antitumor activity. SI-109 effectively inhibits the transcriptional activity of STAT3 (IC50=3 μM). SI-109 and an analog of CRBN ligand lenalidomide have been used to design PROTAC STAT3 degrader SD-36[1].

IC50 & Target[1]

STAT3

9 nM (Ki)

In Vitro

SI-109 exerts a moderate growth inhibitory activity in MOLM-16 cells (IC50=3 μM)[1].
SI-109 is ineffective in inhibition of STAT3 Y705 phosphorylation and in suppression of c-Myc expression at concentrations as high as 10 μM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

835.79

Formula

C₄₀H₄₄F₂N₇O₉P

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (179.47 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1965 mL 5.9824 mL 11.9647 mL
5 mM 0.2393 mL 1.1965 mL 2.3929 mL
10 mM 0.1196 mL 0.5982 mL 1.1965 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 7.5 mg/mL (8.97 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 7.5 mg/mL (8.97 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 7.5 mg/mL (8.97 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
SI-109
Cat. No.:
HY-129603
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