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GSK2256098

GSK2256098
GSK2256098 (GTPL7939) is a small molecule FAK kinase inhibitor.
Catalog No. T2281Cas No. 1224887-10-8
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Purity:99.52%
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GSK2256098

Catalog No. T2281Cas No. 1224887-10-8
GSK2256098 (GTPL7939) is a small molecule FAK kinase inhibitor.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
1 mg$39In Stock
2 mg$55In Stock
5 mg$81In Stock
10 mg$139In Stock
25 mg$276In Stock
50 mg$472In Stock
100 mg$695In Stock
500 mg$1,460In Stock
1 mL x 10 mM (in DMSO)$81In Stock
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Product Introduction

Bioactivity
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)
AliasGSK 2256098, GSK-2256098, GTPL7939
Chemical Properties
Molecular Weight414.89
FormulaC20H23ClN6O2
Cas No.1224887-10-8
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (120.51 mM), Sonication is recommended.
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 76 mg/mL (183.2 mM)
Solution Preparation Table
DMSO/Ethanol
1mg5mg10mg50mg
1 mM2.4103 mL12.0514 mL24.1028 mL120.5139 mL
5 mM0.4821 mL2.4103 mL4.8206 mL24.1028 mL
10 mM0.2410 mL1.2051 mL2.4103 mL12.0514 mL
20 mM0.1205 mL0.6026 mL1.2051 mL6.0257 mL
50 mM0.0482 mL0.2410 mL0.4821 mL2.4103 mL
100 mM0.0241 mL0.1205 mL0.2410 mL1.2051 mL

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