| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
PI4KA (phosphatidylinositol 4-kinase alpha). It also shows activity against PI4KB, PI3KA, PI3KB, PI3KG, and PI3KD, but with significantly lower potency (pIC50 values of 5.9, 5.8, 5.9, 5.9, and 6.4, respectively).
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| ln Vitro |
GSK-F1 is a potent inhibitor of PI4KA with an IC50 of approximately 10 nM (pIC50 = 8.0). It exhibits selectivity for PI4KIIIα over PI4Kβ (IC50 = 1,000 nM), PI3Kα (IC50 = 2,512 nM), PI3Kβ (IC50 = 7,943 nM), PI3Kδ (IC50 = 2,512 nM), and PI4Kγ (IC50 = 2,512 nM). This selectivity profile makes it a valuable tool for studying the specific role of PI4KA in cellular signaling.
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| ln Vivo |
Specific in vivo activity data for GSK-F1 are limited in the available literature. As an orally active compound, it is expected to have good bioavailability. Its in vivo efficacy has been studied in the context of HCV infection research. However, detailed animal model studies, such as those for efficacy in disease models or pharmacokinetic-pharmacodynamic relationships, are not extensively described.
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| Enzyme Assay |
The in vitro enzyme inhibition assay for GSK-F1 typically involves measuring the activity of recombinant PI4KA enzyme in the presence of varying concentrations of the compound. The enzyme is incubated with a substrate (such as ATP and phosphatidylinositol), and the production of phosphatidylinositol 4-phosphate is quantified. The IC50 value is determined from the dose-response curve. Selectivity is assessed by testing the compound against a panel of related kinases under similar assay conditions.
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| Cell Assay |
Specific in vitro cell-based assay protocols for GSK-F1 are not detailed. However, cellular activity can be assessed by measuring the inhibition of PI4KA-dependent signaling pathways. For example, cells can be treated with GSK-F1, and the levels of phosphatidylinositol 4-phosphate or downstream signaling events can be quantified using specific antibodies or biosensors. The compound's effect on cell viability or viral replication (in HCV studies) can also be evaluated.
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| Animal Protocol |
Specific in vivo animal model protocols for GSK-F1 are not described. Given its oral activity, typical studies would involve oral gavage administration in rodents. Animal models of HCV infection or other diseases where PI4KA plays a role could be used to assess efficacy. Endpoints would include measurement of viral load, tissue pathology, and biomarker changes.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for GSK-F1 are not extensively reported. As an orally active compound, it is expected to have favorable absorption and bioavailability. Detailed PK parameters such as half-life, clearance, volume of distribution, and protein binding are not specified in the available literature.
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| Toxicity/Toxicokinetics |
Specific toxicological data for GSK-F1 are not available in the searched literature. As a research compound, its safety profile has not been comprehensively characterized. Toxicity studies would be required to determine its safety margin and potential off-target effects before any clinical application.
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| References | |
| Additional Infomation |
GSK-F1 is primarily a research tool for studying the role of PI4KA in cellular signaling and viral infections, particularly HCV. It is not an approved therapeutic agent. Its high potency and selectivity make it a valuable compound for elucidating PI4KA function and for validating this kinase as a potential drug target.
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| Molecular Formula |
C27H18F5N5O4S
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|---|---|
| Molecular Weight |
603.519941806793
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| Exact Mass |
603.099
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| CAS # |
1402345-92-9
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| Related CAS # |
1402345-92-9 GSK-F1
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| PubChem CID |
57406702
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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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| Boiling Point |
744.3±70.0 °C at 760 mmHg
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| Flash Point |
404.0±35.7 °C
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| Vapour Pressure |
0.0±2.5 mmHg at 25°C
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| Index of Refraction |
1.646
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| LogP |
4.43
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
42
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| Complexity |
1120
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=C(C=C(C=N1)C2=CC3=C(C=C2)N=C(N(C3=O)C4=CC=CC=C4C(F)(F)F)N)S(=O)(=O)NC5=C(C=C(C=C5)F)F
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| InChi Key |
MSRFVAYVUUHQCN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H18F5N5O4S/c1-41-24-23(42(39,40)36-21-9-7-16(28)12-19(21)29)11-15(13-34-24)14-6-8-20-17(10-14)25(38)37(26(33)35-20)22-5-3-2-4-18(22)27(30,31)32/h2-13,36H,1H3,(H2,33,35)
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| Chemical Name |
5-[2-amino-4-oxo-3-[2-(trifluoromethyl)phenyl]quinazolin-6-yl]-N-(2,4-difluorophenyl)-2-methoxypyridine-3-sulfonamide
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~125 mg/mL (~207.12 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6569 mL | 8.2847 mL | 16.5695 mL | |
| 5 mM | 0.3314 mL | 1.6569 mL | 3.3139 mL | |
| 10 mM | 0.1657 mL | 0.8285 mL | 1.6569 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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