| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
Stafib-1 is a selective inhibitor of STAT5b, a member of the Signal Transducer and Activator of Transcription (STAT) family of transcription factors. It targets the SH2 domain of STAT5b, which is essential for its dimerization and transcriptional activity. Stafib-1 has a Ki of 44 nM and an IC50 of 154 nM for STAT5b inhibition. It shows more than 50-fold selectivity over STAT5a. By inhibiting STAT5b, Stafib-1 blocks the transcription of genes involved in cell proliferation, survival, and differentiation. STAT5b is a key driver in certain cancers, making it an important therapeutic target.
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| ln Vitro |
Stafib-1 has selectivity greater than 50 times that of STAT5a and is the first small molecule to inhibit the SH2 domain of STAT5b [1].
In vitro, Stafib-1 is the first small molecule which inhibits the STAT5b SH2 domain with more than 50-fold selectivity over STAT5a. It has an IC50 of 154 nM and a Ki of 44 nM for STAT5b inhibition. The compound is used as a chemical probe in oncology research to study STAT5b-driven tumorigenesis, therapeutic resistance, and targeted drug development. Its high selectivity for STAT5b over STAT5a makes it a valuable tool for dissecting the specific roles of these two closely related transcription factors. |
| ln Vivo |
In vivo studies of Stafib-1 are limited, but the compound is used as a chemical probe to study STAT5b biology. As a selective inhibitor of STAT5b, it has the potential to modulate STAT5b-mediated signaling pathways in vivo. The compound's selectivity and potency make it a promising candidate for preclinical studies in oncology. However, detailed in vivo efficacy data for specific disease models are not widely available. Stafib-1 is primarily used as a research tool to study STAT5b function.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for Stafib-1 typically involve measuring its binding to the STAT5b SH2 domain. Surface plasmon resonance (SPR) or fluorescence polarization assays can be used to determine the binding affinity (Ki). Stafib-1 shows a Ki of 44 nM for the STAT5b SH2 domain. These assays confirm the compound's mechanism of action as a direct inhibitor of STAT5b. The compound's selectivity over STAT5a is also assessed using similar binding assays.
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| Cell Assay |
In vitro cellular assays for Stafib-1 typically involve treating cancer cell lines that depend on STAT5b signaling and measuring downstream effects on STAT5b transcriptional activity. The compound inhibits STAT5b-mediated transcription, leading to reduced expression of STAT5b target genes. Cell viability and proliferation assays can also be performed to assess the functional consequences of STAT5b inhibition. Stafib-1's IC50 of 154 nM for STAT5b inhibition is determined in these cellular assays. These cell-based studies are essential for characterizing the compound's biological activity.
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| Animal Protocol |
In vivo animal models for Stafib-1 may include xenograft tumor models driven by STAT5b signaling. The compound is administered by appropriate routes (e.g., oral or intraperitoneal), and tumor growth inhibition is measured. However, detailed animal protocol information for Stafib-1 is limited in the available literature. The compound is primarily used as a research tool for studying STAT5b biology. Its selectivity and potency make it a valuable probe for in vivo studies of STAT5b function.
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| ADME/Pharmacokinetics |
Stafib-1 has a molecular weight of approximately 588.38 g/mol and a molecular formula of C26H24N2O11P2. It is soluble in DMSO. The compound is typically stored as a powder at -20°C for up to 3 years or at 4°C for 2 years. Its chemical structure and physicochemical properties support its use in both in vitro and in vivo studies. Stafib-1's solubility in DMSO facilitates its formulation for cellular and animal studies. The compound is typically stored under appropriate conditions to maintain stability.
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| Toxicity/Toxicokinetics |
Stafib-1 is a selective inhibitor of STAT5b 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. Stafib-1 is for research use only and is not approved for human therapeutic use. It represents a valuable tool compound for studying STAT5b biology and its role in cancer.
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| References | |
| Additional Infomation |
Stafib-1 (CAS# 1688703-26-5) is a selective inhibitor of the STAT5b SH2 domain, with an IC50 of 154 nM and a Ki of 44 nM. It is the first small molecule to inhibit the SH2 domain of STAT5b with more than 50-fold selectivity over STAT5a. Stafib-1 is a potent, selective small molecule inhibitor of the transcription factor STAT5b. It is widely used as a chemical probe in oncology research to study STAT5b-driven tumorigenesis, therapeutic resistance, and targeted drug development. The compound is for research use only and is not approved for human therapeutic use.
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| Molecular Formula |
C26H24N2O11P2
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| Molecular Weight |
602.42
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| Exact Mass |
602.085
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| CAS # |
1688703-26-5
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| PubChem CID |
122432036
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| Appearance |
White to off-white solid powder
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| Density |
1.6±0.1 g/cm3
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| Index of Refraction |
1.700
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| LogP |
0.09
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
41
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| Complexity |
983
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)NC(=O)C2=CC3=C(C=C2)C=C(C=C3)OCC(=O)NCC4=CC(=C(C=C4)OP(=O)(O)O)OP(=O)(O)O
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| InChi Key |
SMUYYYBDKASIKY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H24N2O11P2/c29-25(27-15-17-6-11-23(38-40(31,32)33)24(12-17)39-41(34,35)36)16-37-22-10-9-18-13-20(8-7-19(18)14-22)26(30)28-21-4-2-1-3-5-21/h1-14H,15-16H2,(H,27,29)(H,28,30)(H2,31,32,33)(H2,34,35,36)
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| Chemical Name |
[4-[[[2-[6-(phenylcarbamoyl)naphthalen-2-yl]oxyacetyl]amino]methyl]-2-phosphonooxyphenyl] dihydrogen phosphate
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| Synonyms |
Stafib1; Stafib 1; Stafib-1
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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 (~166.00 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.15 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 25.0 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: ≥ 2.5 mg/mL (4.15 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 25.0 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: ≥ 2.5 mg/mL (4.15 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 | 1.6600 mL | 8.2999 mL | 16.5997 mL | |
| 5 mM | 0.3320 mL | 1.6600 mL | 3.3199 mL | |
| 10 mM | 0.1660 mL | 0.8300 mL | 1.6600 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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