| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
IC50: 27.44 nM (FAK)[1]
|
|---|---|
| ln Vitro |
FAK-IN-9 (Compound 8f; 72 h) suppresses the growth of MDA-MB-157, MDA-MB-231, and MDA-MB-453 cells wIC50 values of 0.167±0.025, 0.126±0.012, and 0.159±0.017 μM, respectively[1]. In a dose-dependent way, MDA-MB-231 cells release relatively significant levels of NO when exposed to FAK-IN-9 (1-4 μM; 72 h)[1]. The invasion and migration of MDA-MB-231 cells is inhibited by FAK-IN-9 (1-4 μM; 48 h) [1]. FAK-IN-9 (1-4 μM; 72 h) efficiently inhibits the signaling pathway controlled by FAK [1]. FAK-IN-9 (4 μM; 72 h) prevents MDA-MB-231 cells from forming stress fibers (SFs) and focal adhesions (FAs) [1]. In MDA-MB-231 cells, FAK-IN-9 (1-4 μM; 72 h) causes apoptosis [1].
|
| ln Vivo |
FAK-IN-9 (Compound 8f; oral; once daily for 30 days; 15 or 30 mg/kg) suppresses lung metastases of MDA-MB-231 in mice[1].
|
| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: MDA-MB-157, MDA-MB-231, MDA-MB-453 and MCF10A Tested Concentrations: Incubation Duration: 72 h Experimental Results: Inhibited proliferation with IC50s of 0.167±0.025, 0.126±0.012, 0.159±0.017 and 2.401±0.131 μM against MDA-MB-157, MDA-MB-231, MDA-MB-453 and MCF10A, respectively. Cell Invasion Assay[1] Cell Types: MDA-MB-231 cells Tested Concentrations: 1, 2 and 4 μM Incubation Duration: 48 h Experimental Results: The numbers of invasive MDA-MB-231 cells were diminished dose-dependently. Cell Migration Assay [1] Cell Types: MDA-MB-231 cells Tested Concentrations: 1, 2 and 4 μM Incubation Duration: 48 h Experimental Results: Remarkably block the migration of MDA-MB-231 cells in a dose-dependent manner. Western Blot Analysis[1] Cell Types: MDA-MB-231 cells Tested Concentrations: 1, 2 and 4 μM Incubation Duration: 72 h Experimental Results: Potently suppressed the autophosphorylation of Y397 in a dose-dependent manner. diminished the levels of p-AKT, MMP-2 and MMP-9 dose dependently. Apoptosis Analysis[1] Cell Types: MDA-MB-231 cells Tested Concentrations: 1, 2 and 4 |
| Animal Protocol |
Animal/Disease Models: BALB/c nude mice, MDA-MB-231 experimental pulmonary metastasis model[1]
Doses: 15 or 30 mg/kg Route of Administration: po (oral gavage) one time/day for 30 days Experimental Results: Potently decreased the numbers of lung tumor nodules dose- dependently. |
| References |
| Molecular Formula |
C36H38CLN7O8S
|
|---|---|
| Molecular Weight |
764.25
|
| CAS # |
2911655-93-9
|
| Appearance |
Typically exists as solid at room temperature
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 1.3085 mL | 6.5424 mL | 13.0847 mL | |
| 5 mM | 0.2617 mL | 1.3085 mL | 2.6169 mL | |
| 10 mM | 0.1308 mL | 0.6542 mL | 1.3085 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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