| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
FAK-IN-26 (compound A8) has a strong binding affinity for FAK, with a Kd value of 15 μM[1]. FAK-IN-26 (1 μmol/L) exhibits broad-spectrum inhibitory activity against a variety of kinases, with inhibition rates of over 95% against FAK and FYNα[1]. Compared to Defactinib (VS6063), FAK-IN-26 (0.5-10 μM) significantly reduces the viability of A549 and SKOV-3 cells at lower concentrations. FAK-IN-26 (0.2-1.6 μM) dose-dependently reduces the number of cancer stem cells in A549 and SKOV-3 cells[1]. FAK-IN-26 (62.5-1000 nM, 72 h) significantly induces G2/M phase arrest in A549 and SKOV-3 cell lines[1]. FAK-IN-26 (0.1-10 nM, 6-48 h) dose-dependently reduced the migration rate and migration distance of A549 and SKOV-3 cells, with significant inhibitory effects observed at concentrations of 1 nM and 10 nM [1]. FAK-IN-26 (31.25-62.5 nM, 48 h) effectively inhibited FAK autophosphorylation in A549 and SKOV-3 cells in a dose-dependent manner, with better inhibitory effects in A549 cells [1]. FAK-IN-26 exhibited good metabolic stability in human liver microsomes, with CLint and T1/2 of 31.8 μL/min/mg and 43.6 min, respectively [1].
|
|---|---|
| ln Vivo |
FAK-IN-26 (compound A8) (25-50 mg/kg, orally, once or twice daily for five days, followed by a two-day break, for a total of 28 days) showed stronger antitumor activity than Defactinib (VS6063), erlotinib, and paclitaxel in both A549 and SKOV-3 tumor mouse models, and its combination with paclitaxel further enhanced the efficacy of the SKOV-3 tumor model [1]. FAK-IN-26 (500-2000 mg/kg) was well tolerated in mice, and no acute toxicity was observed at the highest dose of 2000 mg/kg [1]. FAK-IN-26 has good tumor absorption and retention properties. It reached a peak absorption of 4.16 ID/g 30 minutes after injection in S180 tumor-bearing mice. It can also effectively penetrate the blood-brain barrier. The brain absorption was 2.63% ID/g at 15 minutes and 1.62% ID/g at 120 minutes [1].
|
| Cell Assay |
Cell cycle analysis [1]
Cell Types: A549 cells, SKOV-3 cells Tested Concentrations: 62.5, 125, 250, 500, 1000 nM Incubation Duration: 72 hours Experimental Results: Significantly arrested A549 cells and SKOV-3 cells in the G2/M phase, with the proportions of A549 cells being 70.8%, 68.7%, 68.8%, 57.9%, and 44.7%, respectively. Cell migration assay [1] Cell Types: A549 cells, SKOV-3 cells Tested Concentrations: 0.1, 1, 10 nM Incubation Duration: 6, 12, 24, 48 hours Experimental Results: The migration rate and distance of A549 and SKOV-3 cells decreased in a dose-dependent manner, with significant inhibition observed at concentrations of 1 nM and 10 nM. Western Blot Analysis [1] Cell Types: A549 cells, SKOV-3 cells Tested Concentrations: 31.25, 62.5 nM Incubation Duration: 48 hours Experimental Results: The expression of p-FAK925 protein in A549 and SKOV-3 cells was effectively inhibited in a dose-dependent manner, and the effect was better in A549 cells. |
| Animal Protocol |
Animal/Disease Models: A549 and KOV-3 cells were subcutaneously injected into Kunming mice until the tumor volume reached 70-100 mm3 [1].
Doses: A549 tumor model: 50 mg/kg, KOV-3 tumor model: 25 mg/kg Route of Administration: Oral (po), A549 tumor model was administered once daily for 5 consecutive days, followed by a 2-day break; KOV-3 tumor model was administered twice daily for 5 consecutive days, followed by a 2-day break, and then the tumor volume and weight were measured. Experimental Results: In the A549 tumor model, the tumor inhibition rate was significantly increased to 59.15%, which was superior to VS6063 (40.69%) and erlotinib (47.41%). In the SKOV-3 tumor model, the tumor inhibition rate reached 57.9%, which was superior to the tumor inhibition rates of VS6063 and paclitaxel (53.89% and 55.30%, respectively). Furthermore, the combination therapy with paclitaxel further enhanced the anti-tumor effect (tumor inhibition rate: 76.63%). |
| References |
| Molecular Formula |
C20H19BRFN5O2
|
|---|---|
| Molecular Weight |
460.30
|
| CAS # |
2801785-12-4
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(NC)C1=CC=CC=C1NC2=NC(NC3=CC=C(OCCF)C=C3)=NC=C2Br
|
| 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 | 2.1725 mL | 10.8625 mL | 21.7250 mL | |
| 5 mM | 0.4345 mL | 2.1725 mL | 4.3450 mL | |
| 10 mM | 0.2172 mL | 1.0862 mL | 2.1725 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
