2. Protein Tyrosine Kinase/RTK Apoptosis
  3. FAK Apoptosis
  4. FAK-IN-2

FAK-IN-2 is a potent and orally active focal adhesion kinase (FAK) inhibitor, with anticancer activity (FAK IC50= 35 nM). FAK-IN-2 covalently inhibits the autophosphorylation of FAK in a dose-dependent manner, and inhibits the clone formation and migration of tumor cells, inducing apoptosis.

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FAK-IN-2 Chemical Structure

FAK-IN-2 Chemical Structure

CAS No. : 2872588-02-6

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Based on 1 publication(s) in Google Scholar

FAK-IN-2 Related Antibodies

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Description

FAK-IN-2 is a potent and orally active focal adhesion kinase (FAK) inhibitor, with anticancer activity (FAK IC50= 35 nM). FAK-IN-2 covalently inhibits the autophosphorylation of FAK in a dose-dependent manner, and inhibits the clone formation and migration of tumor cells, inducing apoptosis[1].

IC50 & Target

IC50: 35 nM (FAK)[1]
In Vitro

FAK-IN-2 (compound 11w) (0-5 μM; 72 hours) has high anti-proliferation activities on cancer cell lines, as well as certain toxicity on normal cell lines[1].
FAK-IN-2 (0-30 nM; 14 days) can remarkably affect HCT-116 cells clone formation in a dose-dependent manner[1].
FAK-IN-2 (10-500 nM; 24 and 48 hours) significantly inhibits the migration of HCT116 cells at both 24 h and 48 h in a dose-dependent manner[1].
FAK-IN-2 (0.001-10 μM; 4 and 24 hours) inhibits the phosphorylation of FAK and its downstream proteins from multiple pathways[1].
FAK-IN-2 (0.01-1 μM; 24 or 48 hours) induces strong cell cycle arrest at the G2/M phase and apoptosis[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

FAK-IN-2 Related Antibodies

Cell Proliferation Assay

Cell Line: Hela, HCT116, MDA-MB-231, H9C2, L929, LO2, HEK293[1]
Concentration: 0-5 μM
Incubation Time: 72 hours
Result: Showed high anti-proliferation activities on cancer cell lines, as well as certain toxicity on normal cell lines.

Western Blot Analysis

Cell Line: HCT116 cells[1]
Concentration: 0.001, 0.01, 0.1, 1 and 10 μM
Incubation Time: 4 and 24 hours
Result: Inhibited the phosphorylation of FAK and its downstream proteins from multiple pathways.

Cell Cycle Analysis

Cell Line: HCT116 cells[1]
Concentration: 0.01, 0.05, 0.1 and 0.5 μM for 24 hours; 0.01, 0.05, 0.1, 0.3 and 1 μM for 48 hours
Incubation Time: 24 and 48 hours
Result: Induced strong cell cycle arrest at the G2/M phase and apoptosis.
In Vivo

FAK-IN-2 (5 and 15 mg/kg; 16 days; once daily) has potent antitumor effects in model mice with a dose-dependent manner without significant toxicity[1] Pharmacokinetic Parameters of FAK-IN-2 in male Sprague-Dawley rats[1].

PO (5 mg/kg) IV (5 mg/kg)
Cmax (μg/L) 239.87 2965.27
Tmax (h) 1.44 0.08
T1/2 (h) 4.70 7.57
Clz (L/h/kg) 9.92 2.19
AUC0-t (μg*h/L) 512.75 2439.06
F % 21.02%

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Balb/C nu/nu mice (HCT116-injected)[1]
Dosage: 5 and 15 mg/kg
Administration: 16 days; once daily
Result: Displayed potent antitumor effects in a dose-dependent manner without significant toxicity.
Molecular Weight

563.05

Formula

C28H31ClN8O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C=CC(N[C@@H](C(N1CCN(CC1)C2=CC=C(C=C2)NC3=NC(NC4=C(C=CC=C4)C(NC)=O)=C(C=N3)Cl)=O)C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (177.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7760 mL 8.8802 mL 17.7604 mL
5 mM 0.3552 mL 1.7760 mL 3.5521 mL
View the 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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C2

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Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (4.44 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.44 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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. 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 1.7760 mL 8.8802 mL 17.7604 mL 44.4010 mL
5 mM 0.3552 mL 1.7760 mL 3.5521 mL 8.8802 mL
10 mM 0.1776 mL 0.8880 mL 1.7760 mL 4.4401 mL
15 mM 0.1184 mL 0.5920 mL 1.1840 mL 2.9601 mL
20 mM 0.0888 mL 0.4440 mL 0.8880 mL 2.2201 mL
25 mM 0.0710 mL 0.3552 mL 0.7104 mL 1.7760 mL
30 mM 0.0592 mL 0.2960 mL 0.5920 mL 1.4800 mL
40 mM 0.0444 mL 0.2220 mL 0.4440 mL 1.1100 mL
50 mM 0.0355 mL 0.1776 mL 0.3552 mL 0.8880 mL
60 mM 0.0296 mL 0.1480 mL 0.2960 mL 0.7400 mL
80 mM 0.0222 mL 0.1110 mL 0.2220 mL 0.5550 mL
100 mM 0.0178 mL 0.0888 mL 0.1776 mL 0.4440 mL
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FAK-IN-2 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FAK-IN-22872588-02-6FAKApoptosisPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseCovalent inhibitorCancerCell proliferationOralInhibitorinhibitorinhibit

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