| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C20H23ClN6O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
GSK2256098 is a selective inhibitor of FAK kinase that suppresses the growth and survival of pancreatic ductal adenocarcinoma cells. It is supplied as a white to yellow solid (C20H23ClN6O2, MW 414.89) at 99.86% purity.
Physical & Chemical Properties
| CAS Number | 1224887-10-8 |
|---|---|
| Molecular Formula | C20H23ClN6O2 |
| Molecular Weight | 414.89 g/mol |
| Purity | 99.86% |
| Appearance | Solid |
| Color | White to yellow |
| SMILES | O=C(NOC)C1=CC=CC=C1NC2=CC(NC3=CC(C)=NN3C(C)C)=NC=C2Cl |
| Signaling Pathway | Protein Tyrosine Kinase/RTK; Apoptosis |
| 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. |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | ≥ 30 mg/mL (72.31 mM) | use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (6.03 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (6.03 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
GSK2256098 is a thousand fold more selective for FAK than for its nearest family member, Pyk2. GSK2256098 inhibits FAK activity by targeting the FAK phosphorylation site tyrosine (Y) 397. In the cancer cell lines OVCAR8 (ovary), U87MG (brain) and A549 (lung), GSK2256098 inhibits FAK activity or Y397 phosphorylation with IC50s of 15, 8.5 and 12 nM, respectively. Across 6 PDAC cell lines, treatment with GSK2256098 (0.1–10 μM) produced FAK Y397 phosphorylation or activity responses spanning a low (less than 20% inhibition) to a high (more than 90% inhibition) level. The least and most sensitive cell lines (PANC-1 and L3.6P1) are chosen for further analysis. In L3.6P1 cells, GSK2256098 inhibition of FAK Y397 phosphorylation correlates with lower levels of phosphorylated Akt and ERK. GSK2256098 reduces cell viability, anchorage-independent growth and motility in a dose-dependent manner[1].
In Vivo
Because FAK is well known to play an important role in angiogenesis, proliferation and apoptosis, tumor samples harvested from the therapy experiments are examined. Tumors from mice treated with GSK2256098 and Paclitaxel show significantly lower microvessel densities by CD31 evaluation than tumors from the vehicle control group (P<0.05). This is consistent across both models, although Ishikawa tumors have the lowest microvessel density. In all tumor models, mice treated with GSK2256098 show less proliferation by Ki67 than control, and Ishikawa tumors have the lowest Ki67 expression in response to therapy. After GSK2256098 treatment, Ishikawa tumors have higher apoptotic indices than Hec1A tumors. Significant rates of apoptosis are seen in all models treated with the combination of GSK2256098 and Paclitaxel[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Cell Assay[1]
Culture PDAC cells in the wells of a 96-well plate. Add ten microliters of MTS to the wells (total volume: 100 μL). Keep the plate in a 37°C incubator for 10-30 min, then read the absorbance of reacted MTS at 450 nm on a microplate reader. Calculate the IC50 of GSK2256098 on cell viability with the Sigma plot program. Culture PDAC cells on a 6-well plate. When cell confluence reaches about 70% in regular medium, incubate the cells for 48 or 72 hr in medium with 0.1-10 μM GSK2256098. Once treatments end, re-seed the cells and keep them for 9 d. Then stain the cells with Clonogenic Reagent and count the blue colonies[1].
Animal Administration[2]
Mice[2] Use athymic nude mice (female, 8- to 12-week-old). For therapeutic experiments, inoculate 4×106 Ishikawa or Hec1A cells into the uterine horn. After tumor cell injection, randomize the mice (n=10 mice per group) into the following groups: group 1 (100 μL of vehicle control; oral, daily); group 2 (75 mg/kg GSK2256098 in 100 μL of vehicle; oral, daily); group 3 (2.5 mg/kg Paclitaxel in 200 μL of PBS; intraperitoneal, weekly); group 4 (GSK2256098 plus Paclitaxel at the doses and frequencies above). Start therapy 10-14 days after tumor injection. Monitor the mice for adverse effects and sacrifice them by cervical dislocation four to six weeks after treatment initiation. At the end of each experiment, record each mouse’s weight, aggregate tumor weight, location and number of tumor nodules for each treatment group. Process tumor samples for further analysis by preserving them in optimal cutting temperature medium for frozen section analysis and fixing them in formalin for paraffin-embedded section analysis.
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Local photocrosslinking of native tissue matrix regulates lung epithelial cell mechanosensing and function. Nat Mater 2025 Sep 5. PMID: 40913159
PTK2/FAK inhibition triggers TMED9-mediated protective autophagy in pancreatic cancer cell via enhancing ERGIC-ERES contact. Autophagy 2026 May 29:1-15. PMID: 42144738
Inhibition of focal adhesion kinase impairs tumor formation and preserves hearing in a murine model of NF2-related schwannomatosis. Sci Adv 2026 Jan 30;12(5):eady8382. PMID: 41616055
Role of the PI3K/AKT signaling pathway in the cellular response to Tumor Treating Fields (TTFields). Cell Death Dis 2025 Mar 27;16(1):210. PMID: 40148314
C1QBP forms a positive feedback loop with the PAICS/FAK/C-MYC axis to promote cancer cell proliferation. Oncogene 2025 Sep 30. PMID: 41028903
Notch controls urothelial integrity in the mouse bladder. JCI Insight 2020 Feb 13;5(3):e133232.
WISP-3 drives LUAD metastasis by suppressing miR-5004-5p to upregulate MMP-12. Biochem Pharmacol 2026 Jun 25;251(Pt 2):118189. PMID: 42349620
TRAF6 promotes spinal microglial M1 polarization to aggravate neuropathic pain by activating the c-JUN/NF-kB signaling pathway. Cell Biol Toxicol 2024 Jul 12;40(1):54. PMID: 38995476
Inhibition of ELOVL6 activity impairs mitochondrial respiratory function and inhibits tumor progression in FGFR3-mutated bladder cancer cells. Biochim Biophys Acta Mol Basis Dis 2025 Aug 18;1871(8):168023. PMID: 40835210
Focal Adhesion Kinase Activation Mediates IQ Motif-Containing GTPase-Activating Protein 3-Promoted Lung Metastasis in Osteosarcoma. Am J Pathol 2026 Jul 28:S0002-9440(26)00202-6. PMID: 42520958
