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SSTC3

Alias: SSTC-3; SSTC 3
Cat No.:V38819 Purity: ≥98%
SSTC3 is an agonist of casein kinase 1α (CK1α) (Kd = 32 nM) and inhibits WNT signaling (EC50 = 30 nM).
SSTC3
SSTC3 Chemical Structure CAS No.: 1242422-09-8
Product category: New2
This product is for research use only, not for human use. We do not sell to patients.
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1mg
5mg
10mg
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Product Description
SSTC3 is an agonist of casein kinase 1α (CK1α) (Kd = 32 nM) and inhibits WNT signaling (EC50 = 30 nM). SSTC3 has minimal gastrointestinal toxicity compared with other types of WNT inhibitors.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
Targeted reduction of HCT116 cell viability occurs with SSTC3 (0-1μM, 5 days). When the mutant CTNNB1 allele that causes its carcinogenic characteristics is removed, this ability is greatly diminished [1].
ln Vivo
A 24-hour course of SSTC3 therapy is possible [1]. In CD-1 mice, the intraperitoneal injection of SSTC3 (25 mg/kg, once daily for 8–12 days) suppresses the progression of colorectal cancer [1]. For a month, SSTC3 (10 mg/kg, intraperitoneally injected once daily) suppresses the growth of tumors caused by Apc mutations [1].
Cell Assay
Cell viability assay[1]
Cell Types: Colorectal cancer (CRC) cell line.
Tested Concentrations: 0-1μM.
Incubation Duration: 5 days.
Experimental Results: diminished vitality.

Western Blot Analysis[1]
Cell Types: SW403 cells.
Tested Concentrations: 100 nM.
Incubation Duration: 15 minutes.
Experimental Results: Increased beta-catenin phosphate levels.
Animal Protocol
Animal/Disease Models: Fiveweeks old Apcmin mice [1].
Doses: 10 mg/kg.
Route of Administration: IP 1 month.
Experimental Results: Inhibition of Apc mutation-driven tumor growth.

Animal/Disease Models: CD-1 mice.
Doses: 25 mg/kg. Management: One IP per day for 8-12 days.
Experimental Results: Inhibition of growth of HCT116 xenografts. attenuated the growth of this metastatic CRC PDX and Dramatically diminished the cell density of residual cancer. The expression of WNT biomarkers in this CRC PDX was diminished.
References

[1]. Differential abundance of CK1α provides selectivity for pharmacological CK1α activators to target WNT-dependent tumors. Sci Signal. 2017 Jun 27;10(485). pii: eaak9916.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H17F3N4O3S2
Molecular Weight
518.5313
Exact Mass
518.069
CAS #
1242422-09-8
PubChem CID
46912682
Appearance
Light yellow to yellow solid powder
LogP
4.3
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
10
Rotatable Bond Count
6
Heavy Atom Count
35
Complexity
823
Defined Atom Stereocenter Count
0
SMILES
S(C1C([H])=C([H])C(C(N([H])C2=NC(=C([H])S2)C2=C([H])C([H])=C([H])C([H])=N2)=O)=C([H])C=1[H])(N(C([H])([H])[H])C1C([H])=C([H])C(C(F)(F)F)=C([H])C=1[H])(=O)=O
InChi Key
HSFAATUFWDDUGW-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H17F3N4O3S2/c1-30(17-9-7-16(8-10-17)23(24,25)26)35(32,33)18-11-5-15(6-12-18)21(31)29-22-28-20(14-34-22)19-4-2-3-13-27-19/h2-14H,1H3,(H,28,29,31)
Chemical Name
4-[methyl-[4-(trifluoromethyl)phenyl]sulfamoyl]-N-(4-pyridin-2-yl-1,3-thiazol-2-yl)benzamide
Synonyms
SSTC-3; SSTC 3
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~125 mg/mL (~241.07 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.01 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.08 mg/mL (4.01 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.9285 mL 9.6426 mL 19.2853 mL
5 mM 0.3857 mL 1.9285 mL 3.8571 mL
10 mM 0.1929 mL 0.9643 mL 1.9285 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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