2. Protein Tyrosine Kinase/RTK
  3. FAK
  4. Y15

Y15  (Synonyms: FAK Inhibitor 14)

Cat. No.: HY-12444 Purity: ≥98.0%
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Y15 is a potent and specific inhibitor of focal adhesion kinase (FAK) that inhibits its autophosphorylation activity, decreases the viability of cancer cells, and blocks tumor growth.

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

Y15 Chemical Structure

Y15 Chemical Structure

CAS No. : 4506-66-5

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Customer Review

Based on 20 publication(s) in Google Scholar

Y15 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Y15 is a potent and specific inhibitor of focal adhesion kinase (FAK) that inhibits its autophosphorylation activity, decreases the viability of cancer cells, and blocks tumor growth.

IC50 & Target

FAK[1]
In Vitro

Y15 directly blocks autophosphorylation activity of FAK. Y15 inhibits Y397 phosphorylation of FAK starting at 0.1 μM in Panc-1 cells. At a dose of 100 μM, Y15 has the same or better inhibition as TAE226. Of note, total FAK is downregulated at higher doses of Y15. Y15 also blocks phosphorylation of the FAK downstream substrate, paxillin. Total paxillin is decreased at higher doses similar to FAK. Thus, Y15 inhibits FAK phosphorylation in a dose-dependent manner[1]. MTS assay is completed using a range of Y15 doses on all cell lines (TT, K1, BCPAP, and TPC1, respectively).Y15 inhibited cell viability in a dose-dependent manner across all thyroid cell lines evaluated. IC50 is 2.05, 5.74, 9.99, and 17.54 μM for TT, TPC1, BCPAP, and K1, respectively[2].
In macrophages treated with Y15, the filopodia and lamellipodia remain mobile. The lawn of particles surrounding macrophages appeared larger in cells treated with Y15[4].

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

Y15 Related Antibodies
In Vivo

Nude mice bearing Panc si-ctrl xenografts are treated with TAE226, a dual FAK and IGF-1R tyrosine kinase inhibitor, to provide a reference for the antitumor effect of dual inhibition of FAK and IGF-1R. Without drug treatment, Panc si5-IGF-1R xenografts grew slower than Panc si-ctrl xenografts (Panc si5-IGF-1R/PBS vs. Panc si-ctrl/PBS), suggesting moderate tumor suppression by inhibiting the IGF-1R pathway only. Further inhibition of FAK activity by Y15 treatment suppresses the growth of Panc si5-IGF-1R xenografts more drastically (Panc si5-IGF-1R/PBS vs. Panc si5-IGF-1R/Y15). A similar antitumor effect is seen in Panc si-ctrl xenografts treated with TAE226 (Panc si5-IGF-1R/Y15 vs. Panc si-ctrl/TAE226). Mice demonstrates normal grooming and eating habits throughout the experiment[3].

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

284.01

Formula

C6H14Cl4N4
CAS No.
Appearance

Solid

Color

Off-white to gray

SMILES

[H]Cl.[H]Cl.[H]Cl.[H]Cl.NC1=CC(N)=C(N)C=C1N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Store at room temperature, keep dry and cool

In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (176.05 mM; ultrasonic and warming and heat to 50°C)

DMSO : 25 mg/mL (88.03 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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5210 mL 17.6050 mL 35.2100 mL
5 mM 0.7042 mL 3.5210 mL 7.0420 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 10 mg/mL (35.21 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: ≥98.0%

SDS (393 KB)

COA (255 KB) HNMR (183 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

10 μCi of [γ-32P]-ATP in a kinase buffer 20 mM HEPES, pH 7.4, 5 mM MgCl2, 5 mM MnCl2, 0.1 mM Na3VO4 with 0.1 μg of purified FAK protein are incubated in a kinase buffer with 10 μCi of [γ-32P]-ATP. The kinase reaction is performed for 5 minutes at room temperature and stopped by addition of 2× Laemmli buffer. Proteins are separated on a Ready SDS-10% PAGE gel, and the phosphorylated enolase is visualized by autoradiography[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

The cells are treated with Y15 or TAE226 at different concentrations for 24 hours. The 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium compound from Promega Viability kit is added, and the cells are incubated at 37°C for 1-2 hours. The optical density on 96-plate is analyzed with a microplate reader at 490 nm to determine cell viability. In addition, cells are stained with trypan blue after 24 hours of treatment with Y15 and the percent of cells that stained positive are determined with a hemacytometer[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

Mice[3]
Six-week-old, female nude mice are used. 5×106 Panc si5-IGF-1R cells are mixed with matrigel and injected subcutaneously into the flank of athymic nude mice (day 0). Animals are randomly divided into two groups on day 7. One group (n=5) received Y15 (30 mg/kg) and the other received PBS as control treatment (n=5). For Panc si-ctrl xenografts, 5×106 Panc si-ctrl cells are mixed with matrigel and injected subcutaneously into the flank of nude mice. These animals are also randomly divided into two groups on day 7, and one group (n=5) received TAE226 (30 mg/kg), the other group received PBS (n=5) as control treatment. The drugs and PBS are administered through intraperitoneal injection in a total volume of 0.1 mL. Tumor sizes are measured every 3 or 4 d in length (mm)×width (mm) starting from day 10. Tumor volume is calculated as volume (cm3)= 1/2×length (cm)×width(cm)2.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 3.5210 mL 17.6050 mL 35.2100 mL 88.0251 mL
5 mM 0.7042 mL 3.5210 mL 7.0420 mL 17.6050 mL
10 mM 0.3521 mL 1.7605 mL 3.5210 mL 8.8025 mL
15 mM 0.2347 mL 1.1737 mL 2.3473 mL 5.8683 mL
20 mM 0.1761 mL 0.8803 mL 1.7605 mL 4.4013 mL
25 mM 0.1408 mL 0.7042 mL 1.4084 mL 3.5210 mL
30 mM 0.1174 mL 0.5868 mL 1.1737 mL 2.9342 mL
40 mM 0.0880 mL 0.4401 mL 0.8803 mL 2.2006 mL
50 mM 0.0704 mL 0.3521 mL 0.7042 mL 1.7605 mL
60 mM 0.0587 mL 0.2934 mL 0.5868 mL 1.4671 mL
80 mM 0.0440 mL 0.2201 mL 0.4401 mL 1.1003 mL
H2O 100 mM 0.0352 mL 0.1761 mL 0.3521 mL 0.8803 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Y15 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:

Y154506-66-5FAK Inhibitor 14Y 15Y-15FAK Inhibitor14FAK Inhibitor-14FAKPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseInhibitorinhibitorinhibit

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