Cat. No.: HY-144448

FAK-IN-2

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Based on 1 publication(s) in Google Scholar

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.

For research use only. We do not sell to patients.

Purity: 98.27%
CAS No.: 2872588-02-6
Formula: C₂₈H₃₁ClN₈O₃
Molecular Weight:563.05

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

FAK-IN-2 Chemical Structure

CAS No.: 2872588-02-6

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

IC₅₀: 35 nM (FAK)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
H9c2	IC₅₀	1.13 μM Compound: 11w	Cytotoxicity against rat H9c2 cells assessed as cell growth inhibition Cytotoxicity against rat H9c2 cells assessed as cell growth inhibition	[PMID: 34757216]
HCT-116	IC₅₀	0.01 μM Compound: 11w	Antiproliferative activity against human HCT-116 cell line assessed as cell growth inhibition Antiproliferative activity against human HCT-116 cell line assessed as cell growth inhibition	[PMID: 34757216]
HEK293	IC₅₀	1.71 μM Compound: 11w	Cytotoxicity against HEK293 cells assessed as cell growth inhibition Cytotoxicity against HEK293 cells assessed as cell growth inhibition	[PMID: 34757216]
HeLa	IC₅₀	0.41 μM Compound: 11w	Antiproliferative activity against human HeLa cell line assessed as cell growth inhibition Antiproliferative activity against human HeLa cell line assessed as cell growth inhibition	[PMID: 34757216]
L02	IC₅₀	5.3 μM Compound: 11w	Cytotoxicity against human L02 cells assessed as cell growth inhibition Cytotoxicity against human L02 cells assessed as cell growth inhibition	[PMID: 34757216]
L929	IC₅₀	2.42 μM Compound: 11w	Cytotoxicity against mouse L929 cells assessed as cell growth inhibition Cytotoxicity against mouse L929 cells assessed as cell growth inhibition	[PMID: 34757216]
MDA-MB-231	IC₅₀	0.11 μM Compound: 11w	Antiproliferative activity against human MDA-MB-231 cell line assessed as cell growth inhibition Antiproliferative activity against human MDA-MB-231 cell line assessed as cell growth inhibition	[PMID: 34757216]

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.

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)
C_max (μg/L)	239.87	2965.27
T_max (h)	1.44	0.08
T_1/2 (h)	4.70	7.57
Clz (L/h/kg)	9.92	2.19
AUC_0-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.

Chemical Information

CAS No. 2872588-02-6
Appearance Solid
Molecular Weight 563.05
Formula C₂₈H₃₁ClN₈O₃
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

Publications (1)

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Journal Impact Factor

J Radiat Res Appl Sci

2026 Mar 28.

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7760 mL

8.8802 mL

17.7604 mL

5 mM

0.3552 mL

1.7760 mL

3.5521 mL

10 mM

0.1776 mL

0.8880 mL

1.7760 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Chen T, et al. Design, synthesis, and biological evaluation of novel covalent inhibitors targeting focal adhesion kinase. Bioorg Med Chem Lett. 2021;54:128433. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) FAK-IN-2

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

FAK-IN-2

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) FAK-IN-2

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

FAK-IN-2 Related Classifications

Cat. No.: HY-144448