2. Protein Tyrosine Kinase/RTK Apoptosis
  3. FAK Apoptosis
  4. GSK2256098

GSK2256098 is a selective FAK kinase inhibitor, which inhibits growth and survival of pancreatic ductal adenocarcinoma cells.

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

GSK2256098 Chemical Structure

GSK2256098 Chemical Structure

CAS No. : 1224887-10-8

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10 mM * 1 mL in DMSO
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Based on 5 publication(s) in Google Scholar

Other Forms of GSK2256098:

GSK2256098 Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK2256098 is a selective FAK kinase inhibitor, which inhibits growth and survival of pancreatic ductal adenocarcinoma cells.

IC50 & Target

FAK[1]
In Vitro

GSK2256098 is a thousand fold more selective for FAK compared to the nearest FAK family member, Pyk2. GSK2256098 inhibits FAK activity through targeting the phosphorylation site of FAK, tyrosine (Y) 397. GSK2256098 inhibits FAK activity or Y397 phosphorylation in cancer cell lines, OVCAR8 (ovary), U87MG (brain), and A549 (lung), at IC50s of 15, 8.5 and 12 nM, respectively. The responses of 6 PDAC cell lines in regards to FAK Y397 phosphorylation or activity to GSK2256098 treatments (0.1–10 μM) ranged from low (less than 20% inhibition) to high (more than 90% inhibition). The least and most sensitive cell lines (PANC-1 and L3.6P1) are selected for further analysis. GSK2256098 inhibition of FAK Y397 phosphorylation correlated with decreased levels of phosphorylated Akt and ERK in L3.6P1 cells. GSK2256098 decreases cell viability, anchorage-independent growth, and motility in a dose dependent manner[1].

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

GSK2256098 Related Antibodies
In Vivo

FAK is well-known to play an important role in angiogenesis, proliferation, and apoptosis, so the tumor samples harvested from the therapy experiments are examined. Evaluating CD31, significantly lower microvessel densities in tumors from mice treated with GSK2256098 and Paclitaxel is observed than in tumors from mice in the vehicle control group (P<0.05). This is consistent across both models, but Ishikawa tumors had the lowest microvessel density. All tumor models in mice treated with GSK2256098 exhibit less proliferation via Ki67 than control. Ishikawa tumors have the lowest Ki67 expression in response to therapy. Ishikawa tumors have higher apoptotic indices than Hec1A tumors after treatment with GSK2256098. Significant rates of apoptosis are seen in all models that had been treated with combination GSK2256098 and Paclitaxel[2].

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

414.89

Formula

C20H23ClN6O2
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(NOC)C1=CC=CC=C1NC2=CC(NC3=CC(C)=NN3C(C)C)=NC=C2Cl
Shipping

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

DMSO : ≥ 30 mg/mL (72.31 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4103 mL 12.0514 mL 24.1028 mL
5 mM 0.4821 mL 2.4103 mL 4.8206 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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 (6.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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 (6.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). 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, . 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

Purity: 99.62%

SDS (392 KB)

COA (253 KB) LCMS (106 KB)

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

PDAC cells are cultured on the wells of a 96-well plate. Ten microliters of MTS is added to the wells (total value: 100 μL). After the plate is kept in a 37°C incubator for 10-30 min, the absorbance at 450 nm wave length of reacted MTS is determined on a microplate reader. The Sigma plot program is used to calculate IC50 of GSK2256098 on cell viability. PDAC cells are cultured on a 6-well plate. When cell confluence reached about 70% in regular medium, the cells are incubated in the medium containing 0.1-10 μM GSK2256098 for 48 or 72 hr. At the end of treatments, cells are re-seeded and kept for 9 d Then, the cells are stained using Clonogenic Reagent, and the blue colonies are counted[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice[2]
Female 8- to 12-week-old athymic nude mice are used. For therapeutic experiments, 4×106 Ishikawa or Hec1A cells are inoculated into the uterine horn. Following tumor cell injection, the mice are randomized (n=10 mice per group) according to the following groups: 1) 100 μL of a vehicle control (oral, daily); 2) 75 mg/kg GSK2256098 in 100 μL of vehicle (oral, daily); 3) 2.5 mg/kg Paclitaxel in 200 μL of PBS (intraperitoneal, weekly); and 4) GSK2256098 and Paclitaxel (doses and frequencies given above). Therapy is initiated 10-14 days after tumor injection. The mice are monitored for adverse effects and sacrificed using cervical dislocation four to six weeks after initiation of treatment. At the completion of each experiment, each mouse’s weight, aggregate tumor weight, location, and number of tumor nodules are recorded for each treatment group. Tumor samples are processed for further analysis via preservation in optimal cutting temperature medium for frozen section analysis as well as fixed in formalin for paraffin-embedded section analysis.

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 1 mM 2.4103 mL 12.0514 mL 24.1028 mL 60.2569 mL
5 mM 0.4821 mL 2.4103 mL 4.8206 mL 12.0514 mL
10 mM 0.2410 mL 1.2051 mL 2.4103 mL 6.0257 mL
15 mM 0.1607 mL 0.8034 mL 1.6069 mL 4.0171 mL
20 mM 0.1205 mL 0.6026 mL 1.2051 mL 3.0128 mL
25 mM 0.0964 mL 0.4821 mL 0.9641 mL 2.4103 mL
30 mM 0.0803 mL 0.4017 mL 0.8034 mL 2.0086 mL
40 mM 0.0603 mL 0.3013 mL 0.6026 mL 1.5064 mL
50 mM 0.0482 mL 0.2410 mL 0.4821 mL 1.2051 mL
60 mM 0.0402 mL 0.2009 mL 0.4017 mL 1.0043 mL
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GSK2256098 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:

GSK22560981224887-10-8GSK 2256098GSK-2256098FAKApoptosisPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseInhibitorinhibitorinhibit

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