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GSK2256098

Catalog No. T2281 CAS 1224887-10-8

Synonyms: GSK 2256098, GSK-2256098, GTPL7939

GSK2256098 (GTPL7939) is a small molecule FAK kinase inhibitor.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

GSK2256098, CAS 1224887-10-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 39.00
2 mg	In stock	$ 55.00
5 mg	In stock	$ 81.00
10 mg	In stock	$ 139.00
25 mg	In stock	$ 276.00
50 mg	In stock	$ 472.00
100 mg	In stock	$ 695.00
500 mg	In stock	$ 1,460.00
1 mL * 10 mM (in DMSO)	In stock	$ 81.00

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Purity: 99.52%

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Description	GSK2256098 (GTPL7939) is a small molecule FAK kinase inhibitor.
Targets&IC50	FAK:0.4 nM(Ki)
In vitro	GSK2256098 has been developed to inhibit FAK activity through targeting the phosphorylation site of FAK, tyrosine (Y) 397. After a 30-min incubation, GSK2256098 inhibits FAK activity or Y397 phosphorylation in cancer cell lines, OVCAR8 (ovary), U87 mg (brain), and A549 (lung), at IC50 values of 15, 8.5 and 12 nM, respectively. In addition, the data suggests that cellular inhibition of FAK by GSK2256098 can occur as early as 30 min in cultured cells and lasts up to 12 hours in mouse tumor xenografts. GSK2256098 inhibition of FAK kinase activity can decrease Akt and ERK activity. PI3K/Akt and ERK signaling contributes to cell survival, implying a pharmacological value of GSK2256098 in attenuation of abnormal survival pathways in specific types of PDAC cells. GSK2256098 can promote apoptosis in L3.6P1 cells through caspase-9/PARP-related pathways. It attenuates abnormal growth and aberrant motility of PDAC cells in a FAK specific manner[1]. GSK2256098 also inhibits growth, migration, and invasion and induces apoptosis in a subset of GBM cell lines[2].
In vivo	Pharmacokinetic (PK) studies in mice and rats with an intact blood brain barrier indicate that the penetration of GSK2256098 into the CNS is poor. However, it achieves concentrations in tumor of patients with GBM(glioblastoma) exceeding those associated with preClinicalal activity[2]. GSK2256098 has an acceptable safety profile, has evidence of target engagement at doses at or below the MTD (maximum tolerated dose), and has Clinicalal activity in patients with mesothelioma, particularly those with merlin loss[3]. In the Ishikawa orthoptopic murine model, treatment with GSK2256098 results in lower tumor weights and fewer metastases than mice inoculated with Hec1A cells. Tumors treated with GSK2256098 have lower microvessel density (CD31), less cellular proliferation (Ki67), and higher apoptosis (TUNEL) rates in the Ishikawa model when compared to the Hec1a model. GSK2256098 may be therapeutically beneficial to patients with PTEN-mutant uterine cancer, and PTEN represents a potential predictive biomarker[4].
Cell Research	PDAC cells are cultured on a 6-well plate. When cell confluence reachs 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. (Only for Reference)

Synonyms	GSK 2256098, GSK-2256098, GTPL7939
Molecular Weight	414.89
Formula	C20H23ClN6O2
CAS No.	1224887-10-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 76 mg/mL (183.2 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 76 mg/mL (183.2 mM)

References and Literature

1. Zhang J, et al. Cell Cycle. 2014, 13(19):3143-9. 2. Paul Mulholland, et al. Neuro Oncol. 2015, 17(Suppl 5): v11. 3. Soria JC, et al. Ann Oncol. 2016, 27(12):2268-2274. 4. Thanapprapasr D, et al. Mol Cancer Ther. 2015, 14(6):1466-75. 5. Auger KR, et al. Eur J Cancer. 2012, 48:118

Citations

1. Zhang P, Cao X, Guan M, et al. CPNE8 Promotes Gastric Cancer Metastasis by Modulating Focal Adhesion Pathway and Tumor Microenvironment. International Journal of Biological Sciences. 2022, 18(13): 4932-4949.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Tyrosine Kinase Inhibitor Library Target-Focused Phenotypic Screening Library NO PAINS Compound Library Apoptosis Compound Library Kinase Inhibitor Library Anti-Cancer Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

GSK2256098 1224887-10-8 Angiogenesis Apoptosis Cytoskeletal Signaling Tyrosine Kinase/Adaptors FAK Focal adhesion kinase PTK2 protein tyrosine kinase 2 GTPL 7939 GSK 2256098 Inhibitor GSK-2256098 GTPL-7939 GTPL7939 inhibit PTK2 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.