2. Protein Tyrosine Kinase/RTK
  3. FAK
  4. ZINC40099027

ZINC40099027 is a selective FAK activator. ZINC40099027 promotes FAK phosphorylation, without activating its paralogs Pyk2 and Src. ZINC40099027 promotes the wound closure of human intestinal epithelial monolayers and the healing of mouse ulcers by activating FAK. ZINC40099027 can be used for diseases related to gastrointestinal mucosal injury research.

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ZINC40099027 Chemical Structure

ZINC40099027 Chemical Structure

CAS No. : 1211825-25-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 2 publication(s) in Google Scholar

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Description

ZINC40099027 is a selective FAK activator. ZINC40099027 promotes FAK phosphorylation, without activating its paralogs Pyk2 and Src. ZINC40099027 promotes the wound closure of human intestinal epithelial monolayers and the healing of mouse ulcers by activating FAK. ZINC40099027 can be used for diseases related to gastrointestinal mucosal injury research[1].

In Vitro

ZINC40099027 (10-1000 nM, 1 h) promotes FAK phosphorylation in Caco-2 intestinal epithelial cells[1].
ZINC40099027 (10 nM; 24 hours) accelerates the wound closure of Caco-2 epithelial monolayers[1].

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

Western Blot Analysis[1]

Cell Line: Caco-2 intestinal epithelial cells
Concentration: 10 nM, 100 nM, 1000 nM
Incubation Time: 1 h
Result: Specifically increased FAK-Tyr 397 phosphorylation within intact cells while activating neither Pyk2, a close paralogue of FAK, nor Src, another key nonreceptor kinase within the focal adhesion complex.
In Vivo

ZINC40099027 (900 µg/kg; intraperitoneal injection; once every 6 hours; treatment for 3 days) promotes intestinal mucosal healing, reduces the ulcer area, increases the immunoreactivity of phosphorylated FAK in the epithelium at the edge of the ulcer, and does not affect the percentage of Ki-67 positive cells in the Acetic acid (HY-Y0319)-induced ischemic ulcer model in mice[1].
ZINC40099027 (900 µg/kg; intraperitoneal injection; once every 6 hours; treatment for 3 days) promotes ulcer healing, reduces the total ulcer area, and has no significant effect on the morphology of the kidneys and liver in the Indomethacin (HY-14397)-induced small intestine injury model in mice[1].

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

Animal Model: C57BL/6J mice (both male and female, 8-10 weeks old), the ischemic ulcer model was induced by placing a 75% Acetic acid-saturated circular filter disk on the antimesenteric serosa of the jejunum for 15 seconds[1]
Dosage: 900 µg/kg
Administration: Intraperitoneal injection, once every 6 hours, for 3 days
Result: Had smaller ulcers than those receiving the DMSO control.
The percentage of wound closure was markedly higher.
Showed higher immunoreactivity for phosphorylated FAK in the epithelium at the edge.
Animal Model: C57BL/6J mice (both male and female, 8-10 weeks old), the Indomethacin-induced ulcer model was induced by subcutaneous injection of 15 mg/kg Indomethacin dissolved in 100% ethanol[1]
Dosage: 900 µg/kg
Administration: Intraperitoneal injection, once every 6 hours, for 3 days
Result: Reduced the total ulcer area compared to the DMSO control.
Molecular Weight

449.47

Formula

C23H26F3N3O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1C(C2=CC=C(OC)C=C2)CCC1)NC3=CC(C(F)(F)F)=CC=C3N4CCOCC4
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 (222.48 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 2.2248 mL 11.1242 mL 22.2484 mL
5 mM 0.4450 mL 2.2248 mL 4.4497 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.

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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 (5.56 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% Corn Oil

    Solubility: 2.5 mg/mL (5.56 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:

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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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
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 2.2248 mL 11.1242 mL 22.2484 mL 55.6211 mL
5 mM 0.4450 mL 2.2248 mL 4.4497 mL 11.1242 mL
10 mM 0.2225 mL 1.1124 mL 2.2248 mL 5.5621 mL
15 mM 0.1483 mL 0.7416 mL 1.4832 mL 3.7081 mL
20 mM 0.1112 mL 0.5562 mL 1.1124 mL 2.7811 mL
25 mM 0.0890 mL 0.4450 mL 0.8899 mL 2.2248 mL
30 mM 0.0742 mL 0.3708 mL 0.7416 mL 1.8540 mL
40 mM 0.0556 mL 0.2781 mL 0.5562 mL 1.3905 mL
50 mM 0.0445 mL 0.2225 mL 0.4450 mL 1.1124 mL
60 mM 0.0371 mL 0.1854 mL 0.3708 mL 0.9270 mL
80 mM 0.0278 mL 0.1391 mL 0.2781 mL 0.6953 mL
100 mM 0.0222 mL 0.1112 mL 0.2225 mL 0.5562 mL
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ZINC40099027 Related Classifications

Keywords:

ZINC400990271211825-25-0ZINC 40099027ZINC-40099027FAKPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinasemucosal healingrestitutionmigrationmedicinal chemistryInhibitorinhibitorinhibit

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