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T3Inh-1

Cat No.:V64400 Purity: ≥98%
T3Inh-1 is a potent and specific inhibitor of ppGalNAc-T3 (IC50=7 µM).
T3Inh-1
T3Inh-1 Chemical Structure CAS No.: 50440-30-7
Product category: Others 12
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
Other Sizes
Official Supplier of:
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Product Description
T3Inh-1 is a potent and specific inhibitor of ppGalNAc-T3 (IC50=7 µM). T3Inh-1 can reduce FGF23 hormone levels in tissue cells and mice without producing any toxic side effects. T3Inh-1 also protects against breast cancer cells. The ppGalNAc-T3 enzyme is involved in at least two important medical pathways: cancer metastasis and the stabilization of FGF23 (which regulates phosphate levels in the blood).
Biological Activity I Assay Protocols (From Reference)
ln Vitro
T3Inh-1 (5 µM; 24-48 hours; 5 µM; MDA-MB231 cells) exhibits remarkable efficacy, exhibiting >80% and 98% inhibition of migration and invasion, respectively, with no appreciable impact on cell proliferation[1]. shows no toxicity and has no effect on the proliferation of HEK cells[1]. The cleavage of FGF23 is increased by T3Inh-1 (HEK cells; 6 hours)[1].
ln Vivo
T3Inh-1 (25 or 50 mg/kg; ip) increases FGF23 cleavage by blocking ppGalNAc-T3-mediated glycan-masking of FGF23[1].
Animal Protocol
Animal/Disease Models: Wild-type C57BL/6 six to eight week old mice[1]
Doses: 25 or 50 mg/kg
Route of Administration: intraperitoneal (ip) injection (Dissolved in DMSO at 25 and 50 mg/ml then further diluted with PEG400 to create 5 and 10 mg/ml stocks for injection)
Experimental Results: Caused a robust and statistically significant increase the ratio of cleaved/intact FGF23 at the tested 25 and 50 mg/kg concentrations.
References
[1]. Song L, et al. Inhibitor of ppGalNAc-T3-mediated O-glycosylation blocks cancer cell invasiveness and lowers FGF23 levels. Elife. 2017;6:e24051. Published 2017 Mar 31.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C27H20N6O3
Molecular Weight
476.49
CAS #
50440-30-7
Appearance
Typically exists as solids (or liquids in special cases) at room temperature
SMILES
[N+](C1=CC=C2C(C(NC3C=CC(C(NC4C=CC(NC5C=CN=CC=5)=CC=4)=O)=CC=3)=CC=N2)=C1)([O-])=O
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: 10 mg/mL (20.99 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 1 mg/mL (2.10 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 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 1 mg/mL (2.10 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.0987 mL 10.4934 mL 20.9868 mL
5 mM 0.4197 mL 2.0987 mL 4.1974 mL
10 mM 0.2099 mL 1.0493 mL 2.0987 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.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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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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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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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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