FAK inhibitor 2
Based on 2 publication(s) in Google Scholar
FAK inhibitor 2 is a potent focal adhesion kinase (FAK) inhibitor with an IC50 of 0.07 nM, with antitumor and anti-angiogenesis activities.
For research use only. We do not sell to patients.
- Purity: 98.26%
- CAS No.: 2354405-14-2
- Formula: C29H33F3N8O2S2
- Molecular Weight:646.75
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications Citing Use of MedChemExpress (MCE) FAK inhibitor 2
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Biological Activity
IC50: 0.07 nM (FAK)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.001 μM
Compound: 14z
|
Antiproliferative activity against human HCT116 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay
Antiproliferative activity against human HCT116 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay
|
[PMID: 31129452] |
| MCF-10A | IC50 |
0.28 μM
Compound: 14z
|
Cytotoxicity against human MCF10A cells assessed as reduction in cell viability after 72 hrs by MTS assay
Cytotoxicity against human MCF10A cells assessed as reduction in cell viability after 72 hrs by MTS assay
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[PMID: 31129452] |
| MCF7 | IC50 |
0.02 μM
Compound: 14z
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Antiproliferative activity against human MCF7 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay
Antiproliferative activity against human MCF7 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay
|
[PMID: 31129452] |
| PC-3 | IC50 |
0.03 μM
Compound: 14z
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Antiproliferative activity against human PC3 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay
Antiproliferative activity against human PC3 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay
|
[PMID: 31129452] |
| Sf9 | IC50 |
0.07 nM
Compound: 14z
|
Inhibition of human recombinant N-terminal His-tagged FAK (393 to 698 residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) peptide as substrate incubated for 60 mins by ADP-Glo assay
Inhibition of human recombinant N-terminal His-tagged FAK (393 to 698 residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) peptide as substrate incubated for 60 mins by ADP-Glo assay
|
[PMID: 31129452] |
| U-87MG ATCC | IC50 |
0.06 μM
Compound: 14z
|
Antiproliferative activity against human U87MG cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay
Antiproliferative activity against human U87MG cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay
|
[PMID: 31129452] |
Chemical Information
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CAS No. 2354405-14-2
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Appearance Solid
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Molecular Weight 646.75
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Formula C29H33F3N8O2S2
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Color White to off-white
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SMILES
O=C(NC)C(C=CC=C1)=C1NC2=C(C(F)(F)F)C=NC(NC3=CC=C(C(N4CCN(C(SCCN(C)C)=S)CC4)=O)C=C3)=N2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (2)
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Journal Impact Factor
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Most Recent
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J Pharm Pharmacol
miR-424-5p reduces 5-fluorouracil resistance possibly by inhibiting Src/focal adhesion kinase signalling-mediated epithelial-mesenchymal transition in colon cancer cells. [Abstract]2021 Jul 7;73(8):1062-1070. PMID: 33793771 -
Solvent & Solubility
DMSO : 100 mg/mL (154.62 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.87 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (270 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5462 mL | 7.7310 mL | 15.4619 mL | 38.6548 mL |
| 5 mM | 0.3092 mL | 1.5462 mL | 3.0924 mL | 7.7310 mL | |
| 10 mM | 0.1546 mL | 0.7731 mL | 1.5462 mL | 3.8655 mL | |
| 15 mM | 0.1031 mL | 0.5154 mL | 1.0308 mL | 2.5770 mL | |
| 20 mM | 0.0773 mL | 0.3865 mL | 0.7731 mL | 1.9327 mL | |
| 25 mM | 0.0618 mL | 0.3092 mL | 0.6185 mL | 1.5462 mL | |
| 30 mM | 0.0515 mL | 0.2577 mL | 0.5154 mL | 1.2885 mL | |
| 40 mM | 0.0387 mL | 0.1933 mL | 0.3865 mL | 0.9664 mL | |
| 50 mM | 0.0309 mL | 0.1546 mL | 0.3092 mL | 0.7731 mL | |
| 60 mM | 0.0258 mL | 0.1288 mL | 0.2577 mL | 0.6442 mL | |
| 80 mM | 0.0193 mL | 0.0966 mL | 0.1933 mL | 0.4832 mL | |
| 100 mM | 0.0155 mL | 0.0773 mL | 0.1546 mL | 0.3865 mL |