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

FAK-IN-2 

Cat. No.: HY-144448
Handling Instructions

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.

FAK-IN-2 Chemical Structure

FAK-IN-2 Chemical Structure

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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].

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)
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%

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

Shipping

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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FAK-IN-2
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HY-144448
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