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STAT5-IN-17f is a novel and potent STAT5 inhibitor that inhibits the phosphorylation and transcriptional activity of STAT5. ith EC50s of 9 μM and 5 μM in K562 and KU812 cells, respectively. It has anticancer effects.
| ln Vitro |
In K562 and KU812 cells, the EC50 values of STAT5-IN-2 are 9 μM and 5 μM, respectively[1]. The EC50 values of induced cell fluorescence were 2.6 μM and 3.5 μM, respectively, for STAT5-IN-2 (100 nM–50 μM; 48 hours) in KG1a and MV-4-11 cells and STAT5-IN-2 (10 μM; 48 hours) in all cell lines (K562, KU812, KG1a, and MV-4-11 cells) [1]. [1] STAT5-IN-2 (10 μM; 24 hours) Boils STAT5 phosphorylation.
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|---|---|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: KG1a and MV-4-11 cell line Tested Concentrations: 100 nM, 10 µM 1]. , 20 µM, 30 µM, 40 µM, 50 µM Incubation Duration: 48 hrs (hours) Experimental Results: Inhibition of cell growth and apoptosis analysis in KG1a and MV-4-11 cell lines [1] Cell Types: K562, KU812, KG1a and MV- 4- 11 cells Tested Concentrations: 10 µM Incubation Duration: 48 hrs (hours) Experimental Results: Significant increase in the number of apoptotic cells. Western Blot Analysis[1] Cell Types: KG1a, MV-4-11 and KU812 Cell Tested Concentrations: 10 µM Incubation Duration: 24 hrs (hours) Experimental Results: Phosphorylation of STAT5 was inhibited, while phosphorylation levels of STAT3, Akt and Erk1/2 were inhibited No effect. |
| References |
| Molecular Formula |
C26H27N3O
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|---|---|
| Molecular Weight |
397.51208615303
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| Exact Mass |
397.215
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| CAS # |
2111834-61-6
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| Related CAS # |
2111834-61-6;
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| PubChem CID |
137628635
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
5.7
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
567
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C1C=CC2=C(C=CN2)C=1)CCN1C2C=CC(C3C=NC=CC=3)=CC=2C(C)(C)CC1
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| InChi Key |
BELIZDRKUICBJC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H27N3O/c1-26(2)10-13-29(14-15-30-22-6-7-24-20(16-22)9-12-28-24)25-8-5-19(17-23(25)26)21-4-3-11-27-18-21/h3-9,11-12,16-18,28H,10,13-15H2,1-2H3
|
| Chemical Name |
1-[2-(1H-indol-5-yloxy)ethyl]-4,4-dimethyl-6-pyridin-3-yl-2,3-dihydroquinoline
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| Synonyms |
STAT5IN17f STAT5-IN-17f STAT5 inhibitor 17f
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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 (~251.57 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.29 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 | 2.5157 mL | 12.5783 mL | 25.1566 mL | |
| 5 mM | 0.5031 mL | 2.5157 mL | 5.0313 mL | |
| 10 mM | 0.2516 mL | 1.2578 mL | 2.5157 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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