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

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

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1 mg USD 750 In-stock
5 mg USD 2200 In-stock
10 mg USD 3500 In-stock
25 mg USD 7000 In-stock
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Based on 1 publication(s) in Google Scholar

SI-109 Related Antibodies

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  • Purity & Documentation

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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].

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

SI-109 Related Antibodies
Molecular Weight

835.79

Formula

C40H44F2N7O9P
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@H](NC([C@@H]1CC[C@H](CCN(C(C)=O)C[C@@H]2NC(C3=CC(C=C(C(F)(P(O)(O)=O)F)C=C4)=C4N3)=O)N1C2=O)=O)CCC(N)=O)NC(C5=CC=CC=C5)C6=CC=CC=C6
Shipping

Shipping with dry ice.
Storage

-80°C, stored under nitrogen
Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (179.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 6 months.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1965 mL 5.9824 mL 11.9647 mL 29.9118 mL
5 mM 0.2393 mL 1.1965 mL 2.3929 mL 5.9824 mL
10 mM 0.1196 mL 0.5982 mL 1.1965 mL 2.9912 mL
15 mM 0.0798 mL 0.3988 mL 0.7976 mL 1.9941 mL
20 mM 0.0598 mL 0.2991 mL 0.5982 mL 1.4956 mL
25 mM 0.0479 mL 0.2393 mL 0.4786 mL 1.1965 mL
30 mM 0.0399 mL 0.1994 mL 0.3988 mL 0.9971 mL
40 mM 0.0299 mL 0.1496 mL 0.2991 mL 0.7478 mL
50 mM 0.0239 mL 0.1196 mL 0.2393 mL 0.5982 mL
60 mM 0.0199 mL 0.0997 mL 0.1994 mL 0.4985 mL
80 mM 0.0150 mL 0.0748 mL 0.1496 mL 0.3739 mL
100 mM 0.0120 mL 0.0598 mL 0.1196 mL 0.2991 mL
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SI-109 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SI-1092429877-30-3SI109SI 109STATLigands for Target Protein for PROTACTarget Protein-binding MoietyInhibitorinhibitorinhibit

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