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Thienopyridone is a novel and potent phosphatase of regenerating liver (PRL) phosphatase inhibitor with anticancer effects. It inhibits PRL with IC50s of 173 nM, 277 nM and 128 nM for PRL-1, PRL-2, and PRL-3, respectively.
| ln Vitro |
In soft agar, tumor anchorage-independent cell growth was significantly inhibited by thinopyridones. HT-29 and RKO cells exhibit thienopyridone's EC50 values of 3.05 μM and 3.29 μM, respectively[1]. In HeLa cells, thienopyridone (1-75 μM; 24 hours) treatment resulted in a dose-dependent rise in total p130Cas. Thienopyridones cause FAK and p130Cas, which results in caspase-mediated bladder cancer. The caspase-8 and PARP pathways are activated by thienopyridone [1]. HUVEC migration is considerably inhibited, but not proliferation, by thinopyridones (3.75-30 μM; 24 hours) [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: RKO and HT-29 cells Tested Concentrations: 0.5 μM, 1.67 μM, 5 μM, 8.33 μM Incubation Duration: 14 days Experimental Results: Measured by colony number or colony size, independent of cancer cell adhesion Demonstrated dose-dependent inhibition of sexual growth. Western Blot Analysis[1] Cell Types: HeLa Cell Tested Concentrations: 1 μM, 5 μM, 10 μM, 25 μM, 50 μM, 75 μM Incubation Duration: 24 hrs (hours) Experimental Results: A dose-dependent downregulation of total p130Cas was observed. |
| References |
| Molecular Formula |
C13H10N2OS
|
|---|---|
| Molecular Weight |
242.296301364899
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| Exact Mass |
242.051
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| CAS # |
1018454-97-1
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| PubChem CID |
91383855
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| Appearance |
Yellow to brown solid powder
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| LogP |
1.7
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
17
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| Complexity |
349
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(=O)NC=C(N)C2SC(C3=CC=CC=C3)=CC1=2
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| InChi Key |
FBVOPOZVLBHOHR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H10N2OS/c14-10-7-15-13(16)9-6-11(17-12(9)10)8-4-2-1-3-5-8/h1-7H,14H2,(H,15,16)
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| Chemical Name |
7-amino-2-phenyl-5H-thieno[3,2-c]pyridin-4-one
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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 : ~5 mg/mL (~20.64 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.58 mM) (saturation unknown) 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.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1271 mL | 20.6356 mL | 41.2712 mL | |
| 5 mM | 0.8254 mL | 4.1271 mL | 8.2542 mL | |
| 10 mM | 0.4127 mL | 2.0636 mL | 4.1271 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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