| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
FT-709 targets USP9X, a deubiquitinating enzyme that removes ubiquitin moieties from substrate proteins, thereby regulating their stability and function. USP9X is involved in various cellular processes including centrosome function, chromosome alignment during mitosis, EGF receptor degradation, chemical sensitization, and circadian rhythms. By inhibiting USP9X with an IC₅₀ of 82 nM, FT-709 promotes the degradation of USP9X substrates, including Makorin and ZNF598, leading to impairment of ribosomal quality control pathways. The compound also reduces CEP55 expression in pancreatic cancer cells.
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| ln Vitro |
In vitro, FT-709 demonstrates potent USP9X inhibition with an IC₅₀ of 82 nM. The compound reduces CEP55 expression in BxPC3 pancreatic cancer cells with an IC₅₀ of 131 nM. FT-709 lowers Makorin and ZNF598 levels, impairing ribosomal quality control pathways. The compound has shown potential in the treatment of diseases associated with dysregulated cellular processes, such as cancer and other proliferative disorders. FT-709 is thought to interfere with the activity of enzymes or signaling networks that promote tumor growth, metastasis, or resistance to chemotherapy.
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| ln Vivo |
In vivo, FT-709 has potential for the treatment of cancer and other proliferative disorders. USP9X inhibition may impair tumor growth, metastasis, and chemoresistance. The compound's effects on ribosomal quality control pathways and CEP55 expression suggest mechanisms that could be exploited for therapeutic benefit. Further in vivo studies are needed to fully characterize the compound's efficacy and safety profile.
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| Enzyme Assay |
In vitro enzyme assays for FT-709 involve measuring USP9X deubiquitinating activity. The standard protocol includes incubating recombinant USP9X with a ubiquitinated substrate or a fluorogenic ubiquitin-AMC substrate in the presence of varying concentrations of FT-709 (0.01-1000 nM). Cleavage of ubiquitin from the substrate releases fluorescence, which is measured over time. IC₅₀ values are calculated from dose-response curves. Selectivity against other deubiquitinating enzymes is assessed using a panel of DUBs.
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| Cell Assay |
Cell-based assays for FT-709 are conducted in BxPC3 pancreatic cancer cells and other cancer cell lines. Cells are treated with FT-709 at concentrations ranging from 0.1-1000 nM for 24-72 hours. USP9X substrate levels (e.g., Makorin, ZNF598, CEP55) are analyzed by western blot. Cell proliferation and viability are assessed by MTT or CellTiter-Glo assays. Apoptosis is evaluated by Annexin V staining and caspase activation. Ribosomal quality control is assessed by measuring ribosome-associated protein levels. The compound's effects on centrosome function and mitotic progression are evaluated by immunofluorescence microscopy.
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| Animal Protocol |
In vivo animal experiments for FT-709 would typically use mouse xenograft models of cancer. Animals would be administered FT-709 via oral gavage or intraperitoneal injection. Tumor volume would be measured periodically, and body weight monitored. At study termination, tumors and tissues would be collected for analysis of USP9X activity, substrate levels, proliferation, and apoptosis. Pharmacokinetic studies would be performed to determine exposure and bioavailability. The compound's effects on tumor growth and chemosensitivity would be evaluated.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for FT-709 are not extensively reported. As a small molecule with a molecular weight of 498.51 g/mol, the compound is expected to have moderate bioavailability. Storage: powder at -20°C for 3 years; in solvent at -80°C for 6 months. Purity is typically ≥98%. The compound appears as a white to yellow solid powder. Further PK studies would be required for comprehensive characterization.
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| Toxicity/Toxicokinetics |
FT-709 is supplied for research use only and is not intended for human administration. Toxicity data are limited, but the compound is used in research on cancer and proliferative disorders. Standard laboratory safety precautions should be followed. No specific toxicological studies have been published. The compound should be handled with care and stored appropriately.
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| References | |
| Additional Infomation |
FT-709 (CAS 2413991-74-7) is a research compound supplied for laboratory use only. It is not an approved drug and has no clinical trial or marketing authorization status. The compound is a potent and selective USP9X inhibitor with an IC₅₀ of 82 nM. It reduces Makorin and ZNF598 levels and impairs ribosomal quality control. Purity is typically ≥98%. The compound appears as a white to yellow solid powder and should be stored at -20°C.
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| Molecular Formula |
C23H22N4O7S
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|---|---|
| Molecular Weight |
498.508384227753
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| Exact Mass |
498.12
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| CAS # |
2413991-74-7
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| Related CAS # |
(R)-FT709;2413991-75-8
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| PubChem CID |
146448154
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| Appearance |
White to yellow solid powder
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| LogP |
-0.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
35
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| Complexity |
967
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C(=O)(N1CC2CN(S(C3=CN=C4OCCOC4=C3)(=O)=O)CC=2C1)[C@@H](O)C1=C2C(=CC=C1)OC(C)=N2
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| InChi Key |
SCFWBZTVFCUBIZ-NRFANRHFSA-N
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| InChi Code |
InChI=1S/C23H22N4O7S/c1-13-25-20-17(3-2-4-18(20)34-13)21(28)23(29)26-9-14-11-27(12-15(14)10-26)35(30,31)16-7-19-22(24-8-16)33-6-5-32-19/h2-4,7-8,21,28H,5-6,9-12H2,1H3/t21-/m0/s1
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| Chemical Name |
(2S)-1-[5-(2,3-dihydro-[1,4]dioxino[2,3-b]pyridin-7-ylsulfonyl)-1,3,4,6-tetrahydropyrrolo[3,4-c]pyrrol-2-yl]-2-hydroxy-2-(2-methyl-1,3-benzoxazol-4-yl)ethanone
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0060 mL | 10.0299 mL | 20.0598 mL | |
| 5 mM | 0.4012 mL | 2.0060 mL | 4.0120 mL | |
| 10 mM | 0.2006 mL | 1.0030 mL | 2.0060 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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