| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
PPARγ
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|---|---|
| ln Vivo |
In a UMUC9 UC xenograft mouse model, FX-909 (0.03-1 mg/kg; BID for 21 days) has anti-cancer properties [1].
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| References | |
| Additional Infomation |
The PPARγ inhibitor FX-909 is an orally administered peroxisome proliferator-activated receptor γ (PPARγ; PPARG) inverse agonist and inhibitor with potential antitumor activity. After oral administration, the PPARG inhibitor FX-909 selectively targets and covalently binds to a region on PPARG isolated from mutation sites. This binding promotes the formation of an inhibitory conformation of PPARG and inhibits its activity. This inhibits basal transcription and ligand-activated transcription of PPARG and blocks the transcription of PPARG-mediated target genes such as FABP4/Fabp4, AGT/Agt, IVT/Ivd, and ARG1/Arg1. This may inhibit the proliferation of tumor cells with excessive PPARG activation. PPARG is a nuclear receptor whose genes are altered in certain tumor cells associated with luminal lineage subtypes, including amplification, missense mutations, and fusions.
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| Molecular Formula |
C17H10F2N2O3S
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|---|---|
| Molecular Weight |
360.334709644318
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| Exact Mass |
360.038
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| CAS # |
2924573-90-8
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| PubChem CID |
167993670
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| Appearance |
White to off-white solid powder
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| LogP |
2.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
25
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| Complexity |
737
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(F)C=C2C(=C(F)C=1)C(=O)C=C(C1=C(C=CC(C#N)=C1)S(=O)(=O)C)N2
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| InChi Key |
RBUBBZVQPHSZEZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H10F2N2O3S/c1-25(23,24)16-3-2-9(8-20)4-11(16)13-7-15(22)17-12(19)5-10(18)6-14(17)21-13/h2-7H,1H3,(H,21,22)
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| Chemical Name |
3-(5,7-difluoro-4-oxo-1H-quinolin-2-yl)-4-methylsulfonylbenzonitrile
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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) |
DMSO: 100 mg/mL (277.52 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.94 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 25.0 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 | 2.7752 mL | 13.8762 mL | 27.7523 mL | |
| 5 mM | 0.5550 mL | 2.7752 mL | 5.5505 mL | |
| 10 mM | 0.2775 mL | 1.3876 mL | 2.7752 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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