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Purity: ≥98%
STX-0119 is a novel and potent STAT3 inhibitor used as an efficient therapeutic to overcome TMZ resistance in recurrent GBM tumors, and could be the next promising compound leading to survival prolongation. STX-0119 demonstrated strong inhibition of the expression of STAT3 target genes (c-myc, survivin, cyclin D1, HIF-1α and VEGF) and stem cell-associated genes (CD44, Nanog, nestin and CD133) as well as the induction of apoptosis in one stem-like cell line.
ln Vitro |
In HEK293 and MDA-MB-468 cells, STX-0119 (10-50 μM; 24 hours) inhibits STAT3 dimerization by directly interacting with the STAT3 protein as opposed to through regulation by upstream regulators like JAK [1]. [1] STX-0119 (10-50 μM; 24 hours) decreases STAT3 target protein expression.
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ln Vivo |
The oral gavage of STX-0119 (160 mg/kg) once day for four days reduces the formation of SCC-3 tumors in mice [1]. Even eight hours after dose, STX-0119 plasma concentrations (160 mg/kg; oral gavage) are still greater than 100 μg/mL (>260 μM) [1].
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Cell Assay |
Western Blot Analysis[1]
Cell Types: MDA-MB-468 Cell Tested Concentrations: 10, 20 and 50 μM Incubation Duration: 24 hrs (hours) Experimental Results: Expression of STAT3 target proteins (i.e. c-myc, cyclin D1 and survivin) was diminished as a function of concentration dependency mode. Does not inhibit the expression of oncoproteins regulated by STAT3. |
Animal Protocol |
Animal/Disease Models: Male BALB/cA-ν/ν nude mice, SCC-3 lymphoma xenograft model [1]
Doses: 160 mg/kg Route of Administration: po (oral gavage), one time/day for 4 days Experimental Results: Significant Inhibition of SCC-3 cell growth on the fourth day. |
References |
Molecular Formula |
C22H14N4O3
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Molecular Weight |
382.37
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Exact Mass |
382.107
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CAS # |
851095-32-4
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Related CAS # |
851095-32-4
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PubChem CID |
4253236
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Appearance |
White to light yellow solid powder
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LogP |
4.87
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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 |
4
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Heavy Atom Count |
29
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Complexity |
570
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Defined Atom Stereocenter Count |
0
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InChi Key |
MNPXTRXFUMGQLK-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C22H14N4O3/c27-20(24-22-26-25-21(29-22)19-11-6-12-28-19)16-13-18(14-7-2-1-3-8-14)23-17-10-5-4-9-15(16)17/h1-13H,(H,24,26,27)
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Chemical Name |
N-[5-(furan-2-yl)-1,3,4-oxadiazol-2-yl]-2-phenylquinoline-4-carboxamide
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Synonyms |
STX0119 STX 0119 STX0119.
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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 : ~13.33 mg/mL (~34.86 mM)
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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 | 2.6153 mL | 13.0763 mL | 26.1527 mL | |
5 mM | 0.5231 mL | 2.6153 mL | 5.2305 mL | |
10 mM | 0.2615 mL | 1.3076 mL | 2.6153 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.