| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
STAT5a 10.9 μM (Ki) STAT5a 22.2 μM (IC50)
Stafia-1 selectively targets the STAT5a isoform, with high selectivity over STAT5b and other STAT family members. It inhibits STAT5a with a Ki of 10.9 μM and an IC50 of 22.2 μM. The mechanism of action involves binding to the SH2 domain of STAT5a, preventing its phosphorylation, dimerization, and nuclear translocation. This selectivity allows researchers to specifically investigate STAT5a-mediated signaling pathways without the confounding effects of STAT5b inhibition. |
|---|---|
| ln Vitro |
Stafia-1 has greater selectivity against other members of the STAT family and at least a 9-fold selectivity over STAT5b[1].
Stafia-1 demonstrates potent and selective inhibition of STAT5a with a Ki of 10.9 μM and an IC50 of 22.2 μM. It displays high selectivity over STAT5b and other STAT family members, making it a unique tool for studying STAT5a-specific functions. The compound's selectivity profile is particularly valuable for distinguishing the roles of STAT5a versus STAT5b in hematopoietic cell development, immune responses, and cancer progression. In vitro studies typically assess its effects on STAT5a phosphorylation and downstream target gene expression. |
| ln Vivo |
In vivo activity data for Stafia-1 are limited. As a first-in-class STAT5a-selective inhibitor, its primary application has been in vitro biochemical and cellular studies. The compound's selectivity and potency make it a valuable tool for validating STAT5a as a therapeutic target. Further research is needed to evaluate its pharmacokinetic properties and efficacy in animal models. The development of more drug-like derivatives based on Stafia-1 may enable future in vivo studies.
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| Enzyme Assay |
The in vitro enzyme/receptor binding (cell-free) assay for Stafia-1 typically involves a fluorescence polarization-based competition assay using a fluorescently labeled phosphopeptide probe that binds to the SH2 domain of STAT5a. Recombinant STAT5a protein is incubated with varying concentrations of Stafia-1 and the probe. The decrease in fluorescence polarization signal, indicating displacement of the probe by the compound, is measured to calculate the Ki and IC50 values. Selectivity over STAT5b and other STAT family members is assessed using similar assays with the respective proteins.
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| Cell Assay |
The in vitro cellular assay for Stafia-1 typically uses cells expressing STAT5a, such as hematopoietic cell lines. Cells are treated with varying concentrations of Stafia-1, and STAT5a phosphorylation is measured by Western blot using phospho-specific antibodies. STAT5a-dependent transcriptional activity can be assessed using a STAT5-responsive luciferase reporter gene assay. The compound's selectivity for STAT5a over STAT5b can be confirmed in cells expressing only one isoform or by comparing the effects on STAT5a versus STAT5b target genes.
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| Animal Protocol |
In vivo animal studies for Stafia-1 are not extensively documented. As a first-in-class STAT5a-selective inhibitor, its primary use has been as a research tool for in vitro studies. For compounds targeting STAT5, typical in vivo models include xenograft tumors in immunodeficient mice or models of hematological malignancies where STAT5a is known to play a role. However, specific protocols for Stafia-1 in animal models have not been reported. Researchers should perform their own in vivo studies to evaluate its efficacy.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Stafia-1 are not extensively reported. As a research tool compound, detailed ADME parameters including oral bioavailability, half-life, and clearance have not been characterized. The compound has a molecular weight of 506.44 and a formula of C24H27O10P. It is soluble in DMSO and can be formulated for various applications. Researchers should perform their own pharmacokinetic studies if in vivo application is intended.
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| Toxicity/Toxicokinetics |
Toxicity data for Stafia-1 are not available in the public domain. As a research compound, comprehensive toxicological evaluations have not been performed. The compound is intended for laboratory research use only and should be handled with standard safety precautions. Appropriate personal protective equipment should be worn when handling this compound. Consult the Material Safety Data Sheet for specific safety and handling information.
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| References | |
| Additional Infomation |
Stafia-1 is the first potent and selective STAT5a inhibitor, displaying high selectivity over STAT5b and other STAT family members. It inhibits STAT5a with a Ki of 10.9 μM and an IC50 of 22.2 μM. The compound serves as a valuable chemical probe for dissecting the distinct biological functions of STAT5a versus STAT5b. Stafia-1 is not in clinical trials and has not been approved for therapeutic use. It remains an experimental tool for basic research into STAT5a biology and the development of more potent and drug-like STAT5a inhibitors.
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| Molecular Formula |
C24H27O10P
|
|---|---|
| Molecular Weight |
506.44
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| Exact Mass |
506.134
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| CAS # |
2582757-90-0
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| PubChem CID |
146681206
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| Appearance |
White to off-white solid powder
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| LogP |
3.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
35
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| Complexity |
617
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OP(O)(OC1=CC(C2C=C(OC)C(OC)=C(OC)C=2)=CC(C2C=C(OC)C(OC)=C(C=2)OC)=C1)=O
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| InChi Key |
UGUOUFLCZFMHNI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H27O10P/c1-28-19-10-16(11-20(29-2)23(19)32-5)14-7-15(9-18(8-14)34-35(25,26)27)17-12-21(30-3)24(33-6)22(13-17)31-4/h7-13H,1-6H3,(H2,25,26,27)
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| Chemical Name |
[3,5-bis(3,4,5-trimethoxyphenyl)phenyl] dihydrogen phosphate
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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: 250 mg/mL (493.64 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.11 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.11 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9746 mL | 9.8728 mL | 19.7457 mL | |
| 5 mM | 0.3949 mL | 1.9746 mL | 3.9491 mL | |
| 10 mM | 0.1975 mL | 0.9873 mL | 1.9746 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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