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Purity: ≥98%
| Targets |
STX-0119 is a selective inhibitor of STAT3 dimerization, targeting the STAT3 signaling pathway. It binds to the STAT3-SH2 domain and inhibits STAT3 transcription. STAT3 is a transcription factor that plays a critical role in cell proliferation, survival, and angiogenesis. By inhibiting STAT3 dimerization and transcription, STX-0119 disrupts the aberrant activation of STAT3, which is implicated in various cancers and inflammatory diseases. The compound has demonstrated strong inhibition of the expression of STAT3 target genes (c-myc, etc.).
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| 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.
In vitro, STX-0119 (10-50 μM; 24 h) inhibits STAT3 dimerization through direct interaction with the STAT3 protein. It inhibits STAT3 transcription in STAT3-dependent luciferase reporter gene assays in HeLa cells with an IC50 of 74 μM. The compound demonstrates strong inhibition of the expression of STAT3 target genes (c-myc). Its in vitro activity is characterized by potent inhibition of STAT3 dimerization and transcriptional activity. |
| 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].
In vivo, STX-0119 has demonstrated orally bioavailable antitumor activity in xenograft models. It has also shown antifibrotic and anti-inflammatory activity in rodent models of kidney fibrosis, liver fibrosis, and osteoarthritis. As a selective STAT3 inhibitor, it has the potential to overcome TMZ resistance in recurrent GBM tumors. Its in vivo efficacy is attributed to its ability to inhibit STAT3 signaling and modulate gene expression. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for STX-0119 typically involve measuring its binding to the STAT3 SH2 domain. Surface plasmon resonance (SPR) or fluorescence polarization assays can be used to determine the binding affinity. These assays confirm the compound's mechanism of action as a STAT3 dimerization inhibitor. The compound's selectivity for STAT3 over other STAT family members can also be assessed.
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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. In vitro cellular assays for STX-0119 typically involve treating cancer cell lines with the compound and measuring STAT3 transcriptional activity using luciferase reporter gene assays. The compound inhibits STAT3 transcription with an IC50 of 74 μM. Western blotting can be used to assess the compound's effects on STAT3 phosphorylation and the expression of STAT3 target genes. These cell-based studies demonstrate the compound's functional inhibition of STAT3 signaling. |
| 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. In vivo animal models for STX-0119 include xenograft tumor models to evaluate its antitumor activity. The compound is administered orally, and tumor growth inhibition is measured. STX-0119 has demonstrated orally bioavailable antitumor activity in xenograft models. It has also shown antifibrotic and anti-inflammatory activity in rodent models of kidney fibrosis, liver fibrosis, and osteoarthritis. These studies provide evidence for the compound's in vivo efficacy in various disease models. |
| ADME/Pharmacokinetics |
STX-0119 has a molecular formula of C26H25N3O5S and a molecular weight of 491.56 g/mol. The compound is typically stored under appropriate conditions to maintain stability. Its physicochemical properties support its use in both in vitro and in vivo studies. STX-0119's solubility and formulation for administration should be optimized based on specific experimental requirements. The compound is a selective, orally active STAT3 dimerization inhibitor.
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| Toxicity/Toxicokinetics |
STX-0119 is a STAT3 inhibitor with a well-characterized mechanism of action. As with any inhibitor of transcription factors, potential toxicity may include effects on normal gene expression and cellular function. The compound's safety profile should be evaluated in preclinical toxicology studies. STX-0119 is for research use only and is not approved for human therapeutic use. It represents a valuable tool for studying STAT3 biology and its role in cancer and inflammatory diseases.
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| References | |
| Additional Infomation |
STX-0119 (CAS# 851095-32-4) is a selective, orally active STAT3 dimerization inhibitor that suppresses STAT3 transcription with an IC50 of 74 μM. It is a potent STAT3 inhibitor used as an efficient therapeutic to overcome temozolomide (TMZ) resistance in recurrent glioblastoma (GBM) tumors. STX-0119 binds to the STAT3-SH2 domain and inhibits STAT3 transcription. It has demonstrated orally bioavailable antitumor activity in xenograft models and antifibrotic and anti-inflammatory activity in rodent models. The compound is for research use only and is not approved for human therapeutic use.
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| 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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| SMILES |
C1=CC=C(C=C1)C2=NC3=CC=CC=C3C(=C2)C(=O)NC4=NN=C(O4)C5=CC=CO5
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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.
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