| Size | Price | Stock | Qty |
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| 10mg |
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| Other Sizes |
| Targets |
FAK-IN-15 targets focal adhesion kinase (FAK, PTK2). It inhibits FAK kinase activity with an extremely high potency, as reflected by its IC50 value of 0.2691 nM. This exceptional potency makes it one of the most potent FAK inhibitors reported. By inhibiting FAK, the compound disrupts integrin-mediated signaling, which is essential for cell adhesion and migration.
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| ln Vitro |
In vitro, FAK-IN-15 is an extremely potent FAK inhibitor with an IC50 of 0.2691 nM. It exhibits antitumor activity against the U87-MG glioblastoma cell line with an IC50 value of 1.033 μM. This indicates that while it is highly potent against the isolated enzyme, its cellular potency is somewhat lower, likely due to factors such as cell permeability or protein binding. It is expected to inhibit FAK-mediated signaling pathways in various cancer cell types.
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| ln Vivo |
Specific in vivo activity data for FAK-IN-15 are not detailed in the available literature. However, its potent in vitro activity against FAK and its antitumor activity against glioblastoma cells suggest that it would have significant efficacy in vivo. It is expected to be evaluated in mouse xenograft models of various cancers, particularly those that are dependent on FAK signaling.
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| Enzyme Assay |
Non-cellular enzyme assays are used to characterize the inhibitory activity of FAK-IN-15 against FAK. In these assays, the compound is incubated with purified FAK kinase and a peptide substrate in the presence of ATP. The inhibition of phosphorylation is quantified, and the IC50 value is determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays are used to evaluate the antiproliferative and mechanistic effects of FAK-IN-15. Cancer cell lines, such as U87-MG glioblastoma cells, are treated with the compound. Cell viability is assessed using standard assays such as MTT or CellTiter-Glo. The compound's effect on FAK phosphorylation and downstream signaling pathways, such as the PI3K/AKT and MAPK pathways, is evaluated by Western blotting.
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| Animal Protocol |
In vivo animal experiments for FAK-IN-15 would typically be conducted in mouse xenograft models. Immunodeficient mice would be implanted with human cancer cells, and FAK-IN-15 would be administered via intraperitoneal (IP) or oral (PO) routes. Tumor growth inhibition would be the primary endpoint, and tumor tissues would be analyzed for FAK phosphorylation and downstream signaling to confirm target engagement.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties for FAK-IN-15 are not detailed in the available sources. As a small molecule, its PK would be influenced by factors such as solubility, metabolic stability, and permeability. Its properties would be characterized in preclinical studies.
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| Toxicity/Toxicokinetics |
Toxicological data for FAK-IN-15 are not provided in the available sources. As a research compound, its safety profile has not been extensively characterized.
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| References | |
| Additional Infomation |
FAK-IN-15 is a highly potent and selective FAK inhibitor with antitumor activity. It is a valuable tool for cancer research and is not approved for clinical use.
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| Molecular Formula |
C21H24CLN7OS
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|---|---|
| Molecular Weight |
457.98
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| Appearance |
Typically exists as solid at room temperature
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.1835 mL | 10.9175 mL | 21.8350 mL | |
| 5 mM | 0.4367 mL | 2.1835 mL | 4.3670 mL | |
| 10 mM | 0.2184 mL | 1.0918 mL | 2.1835 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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