| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Fat mass and obesity-associated protein (FTO).
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|---|---|
| ln Vitro |
FTO-IN-3 potently and selectively inhibits FTO's RNA demethylase activity, leading to increased m6A levels on mRNA transcripts involved in stem cell maintenance. The exact IC50 has not been publicly disclosed, but it is reported to selectively impair self-renewal in glioblastoma stem cells in vitro. It suppresses the self-renewal capacity of GSCs without affecting normal neural stem cells.
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| Enzyme Assay |
The FTO demethylase activity assay is performed using recombinant FTO enzyme and an RNA oligonucleotide substrate containing N6-methyladenosine (m6A). The compound is pre-incubated with FTO, the RNA substrate, and cofactors (alpha-ketoglutarate, Fe2+, ascorbate). After incubation, the demethylation of m6A is detected and quantified by LC-MS/MS, fluorescence-based assays, or by using a demethylation-specific antibody.
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| Cell Assay |
The primary assay uses patient-derived glioblastoma stem cells (GSCs) grown as neurospheres. Cells are treated with FTO-IN-3 at various concentrations (e.g., 1, 5, 10 uM) for several days. Self-renewal capacity is assessed using limiting dilution assays and neurosphere formation frequency (NFF) quantification. Cell viability is measured by CellTiter-Glo, and differentiation is assessed by staining with neural lineage markers (e.g., GFAP, Tuj1).
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| Animal Protocol |
In vivo studies are conducted in mouse orthotopic xenograft models of glioblastoma. GSCs are implanted intracranially into immunocompromised mice. The compound is administered intraperitoneally or orally daily. Tumor growth is monitored by bioluminescence imaging or MRI. Endpoints include tumor burden, animal survival, and molecular analysis of m6A levels in tumor tissues. Detailed published in vivo data may be limited.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic data are not publicly available for FTO-IN-3. As a small molecule (MW 258.3 g/mol), its ability to cross the blood-brain barrier is an important characteristic. Its absorption, distribution, metabolism, and excretion (ADME) properties would need to be characterized in standard preclinical PK studies using rodents.
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| Toxicity/Toxicokinetics |
No detailed toxicology data are publicly available for FTO-IN-3. As a research chemical targeting a stem cell population, potential effects on normal neural stem cells and other proliferative tissues would need to be evaluated. Standard cytotoxicity and genotoxicity assays (e.g., Ames test) are recommended.
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| References | |
| Additional Infomation |
FTO-IN-3 is a research chemical, not an approved drug. It is a selective FTO inhibitor that impairs self-renewal in glioblastoma stem cells (GSCs) without affecting normal neural stem cells, making it a promising lead for developing brain cancer therapeutics. It is used as a chemical probe to study FTO-driven cancer stem cell biology and the role of m6A RNA methylation in glioblastoma.
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| Molecular Formula |
C12H10N4OS
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|---|---|
| Molecular Weight |
258.30
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| Exact Mass |
258.057
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| CAS # |
2585198-87-2
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| PubChem CID |
156278174
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| Appearance |
White to light yellow solid powder
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| LogP |
2.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
18
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| Complexity |
285
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C2=CC(C3=CN=C(OC)N=C3)=CC=C2N=C1N
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| InChi Key |
POOYWDOOHWPQCU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H10N4OS/c1-17-12-14-5-8(6-15-12)7-2-3-9-10(4-7)18-11(13)16-9/h2-6H,1H3,(H2,13,16)
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| Chemical Name |
6-(2-methoxypyrimidin-5-yl)-1,3-benzothiazol-2-amine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~25 mg/mL (~96.8 mM; ultrasonic and warming and adjust pH to 2 with 1M HCl and heat to 80°C)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (9.68 mM) 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; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. Solubility in Formulation 2: 2.5 mg/mL (9.68 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8715 mL | 19.3573 mL | 38.7147 mL | |
| 5 mM | 0.7743 mL | 3.8715 mL | 7.7429 mL | |
| 10 mM | 0.3871 mL | 1.9357 mL | 3.8715 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.
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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