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| Targets |
STAT5-IN-17f is a potent and selective inhibitor of STAT5, a member of the Signal Transducer and Activator of Transcription (STAT) family. It specifically targets the STAT5 SH2 domain to block phosphorylation and subsequent transcriptional activity. The compound inhibits STAT5 phosphorylation and transcriptional activity without affecting STAT3, AKT, or Erk1/2 phosphorylation. STAT5 is a key transcription factor involved in cell proliferation, survival, and differentiation, and its aberrant activation is implicated in leukemia and other cancers.
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| 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.
In vitro, STAT5-IN-17f inhibits the growth of acute and chronic myeloid leukemia cells. It inhibits KU812 and K562 cell growth with IC50s of 9 and 5 μM, respectively, demonstrating highly potent antileukemic effects. The compound shows minimal effects on bone marrow stromal cells, indicating some selectivity for leukemic cells. Its in vitro activity is characterized by potent inhibition of STAT5 phosphorylation and transcriptional activity in leukemia cell lines. STAT5-IN-17f is a novel and potent STAT5 inhibitor. |
| ln Vivo |
In vivo studies of STAT5-IN-17f are limited, but the compound has the potential to inhibit tumor growth in animal models of leukemia. As a selective inhibitor of STAT5, it may block STAT5-mediated signaling pathways that drive leukemic cell proliferation and survival. The compound's in vivo efficacy would depend on its pharmacokinetic properties and ability to reach target tissues. However, detailed in vivo efficacy data for specific disease models are not widely available. STAT5-IN-17f is primarily used as a research tool.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for STAT5-IN-17f typically involve measuring its binding to the STAT5 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 direct inhibitor of STAT5. The compound's selectivity over STAT3 is also assessed using similar binding assays.
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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. In vitro cellular assays for STAT5-IN-17f typically involve treating leukemia cell lines such as K562 and KU812 with the compound and measuring cell viability, proliferation, and apoptosis. The compound inhibits KU812 and K562 cell growth with IC50s of 9 and 5 μM, respectively. Western blotting can be used to assess the compound's effects on STAT5 phosphorylation and the expression of STAT5 target genes. These cell-based studies demonstrate the compound's antileukemic effects and its mechanism of action as a STAT5 inhibitor. |
| Animal Protocol |
In vivo animal models for STAT5-IN-17f may include xenograft tumor models using leukemia cell lines such as K562 or KU812. The compound is administered by appropriate routes (e.g., oral or intraperitoneal), and tumor growth inhibition is measured. However, detailed animal protocol information for STAT5-IN-17f is limited in the available literature. The compound is primarily used as a research tool for studying STAT5 biology in leukemia.
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| ADME/Pharmacokinetics |
STAT5-IN-17f has a molecular formula of C26H27N3O and a molecular weight of 397.51 g/mol. Its chemical structure supports its use as a small-molecule inhibitor of STAT5. 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. STAT5-IN-17f's solubility and formulation for administration should be optimized based on specific experimental requirements.
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| Toxicity/Toxicokinetics |
STAT5-IN-17f is a potent and selective inhibitor of STAT5 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. STAT5-IN-17f is for research use only and is not approved for human therapeutic use. It represents a valuable tool compound for studying STAT5 biology and its role in leukemia.
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| References | |
| Additional Infomation |
STAT5-IN-17f (CAS# 2111834-61-6), also known as STAT5 inhibitor 17f, is a novel, potent, and selective inhibitor of the phosphorylation and transcriptional activity of STAT5, but not STAT3, AKT, or Erk1/2 phosphorylation. It inhibits KU812 and K562 cell growth with IC50s of 9 and 5 μM, respectively, demonstrating highly potent antileukemic effects with minimal effects on bone marrow stromal cells. STAT5-IN-17f targets the STAT5 SH2 domain to block phosphorylation and subsequent transcriptional activity. The compound is for research use only and is not approved for human therapeutic use.
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| 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
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| 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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