GSK2256098

製品コードS8523 バッチS852302

印刷

化学情報

Synonyms

GTPL7939

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₀H₂₃ClN₆O₂

分子量

414.89

CAS No.

1224887-10-8

Solubility (25°C)*

体外

DMSO

200 mg/mL (482.05 mM)

Ethanol

82 mg/mL (197.64 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	10.000mg/ml (24.10mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	GSK2256098 is a potent, selective, reversible, and ATP competitive FAK kinase inhibitor with apparent Ki of 0.4 nM. GSK2256098 inhibits cancer cell growth and induces apoptosis.
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, this compound inhibits FAK activity or Y397 phosphorylation in cancer cell lines, OVCAR8 (ovary), U87MG (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 this chemical can occur as early as 30 min in cultured cells and lasts up to 12 hours in mouse tumor xenografts. Its 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 this compound in attenuation of abnormal survival pathways in specific types of PDAC cells. It 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]. This compound 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 preclinical activity^[2]. This compound has an acceptable safety profile, has evidence of target engagement at doses at or below the MTD (maximum tolerated dose), and has clinical activity in patients with mesothelioma, particularly those with merlin loss^[3]. In the Ishikawa orthoptopic murine model, treatment with this compound results in lower tumor weights and fewer metastases than mice inoculated with Hec1A cells. Tumors treated with this chemical have lower microvessel density (CD31), less cellular proliferation (Ki67), and higher apoptosis (TUNEL) rates in the Ishikawa model when compared to the Hec1a model. It may be therapeutically beneficial to patients with PTEN-mutant uterine cancer, and PTEN represents a potential predictive biomarker^[4].

製品説明

GSK2256098 is a potent, selective, reversible, and ATP competitive FAK kinase inhibitor with apparent Ki of 0.4 nM. GSK2256098 inhibits cancer cell growth and induces apoptosis.

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, this compound inhibits FAK activity or Y397 phosphorylation in cancer cell lines, OVCAR8 (ovary), U87MG (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 this chemical can occur as early as 30 min in cultured cells and lasts up to 12 hours in mouse tumor xenografts. Its 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 this compound in attenuation of abnormal survival pathways in specific types of PDAC cells. It 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].

This compound 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 preclinical activity^[2].

This compound has an acceptable safety profile, has evidence of target engagement at doses at or below the MTD (maximum tolerated dose), and has clinical activity in patients with mesothelioma, particularly those with merlin loss^[3].

In the Ishikawa orthoptopic murine model, treatment with this compound results in lower tumor weights and fewer metastases than mice inoculated with Hec1A cells. Tumors treated with this chemical have lower microvessel density (CD31), less cellular proliferation (Ki67), and higher apoptosis (TUNEL) rates in the Ishikawa model when compared to the Hec1a model. It may be therapeutically beneficial to patients with PTEN-mutant uterine cancer, and PTEN represents a potential predictive biomarker^[4].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	PDAC(pancreatic ductal adenocarcinoma) cells
	濃度	0.1–10 μM
	反応時間	48 or 72 h
	実験の流れ	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.
動物実験	動物モデル	athymic nude mice
	投薬量	75 mg/kg
	投与方法	oral administration

参考

https://pubmed.ncbi.nlm.nih.gov/25486573/
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4638528/
https://pubmed.ncbi.nlm.nih.gov/27733373/

https://pubmed.ncbi.nlm.nih.gov/25833835/
http://www.ejcancer.com/article/S0959-8049(12)72185-8/pdf

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Focal adhesion kinase plays an essential role in Th17 cell differentiation by stimulating NF-κB signaling [ Front Immunol, 2025, 16:1596802]	PubMed: 41050684
Injured tubular epithelia-derived CCN1 promotes the mobilization of fibroblasts toward injury sites after kidney injury [ iScience, 2025, 28(4):112176]	PubMed: 40224016
Injured tubule derived CCN1 exacerbates renal congestion-mediated acute kidney injury and fibrosis [ Sci Rep, 2025, 15(1):20840]	PubMed: 40594194
DNA hypomethylator phenotype reprograms glutamatergic network in receptor tyrosine kinase gene-mutated glioblastoma [ Acta Neuropathol Commun, 2024, 12(1):40]	PubMed: 38481314
FAK suppresses antigen processing and presentation to promote immune evasion in pancreatic cancer [ Gut, 2023, gutjnl-2022-327927]	PubMed: 36977556
FAK suppresses antigen processing and presentation to promote immune evasion in pancreatic cancer [ Gut, 2023, 1–2]	PubMed: None
YAP Inactivation by Soft Mechanotransduction Relieves MAFG for Tumor Cell Dedifferentiation [ Research (Wash D C), 2023, 6:0215]	PubMed: 37614365
YAP Inactivation by Soft Mechanotransduction Relieves MAFG for Tumor Cell Dedifferentiation [ Research -Wash D C), 2023, 6:0215]	PubMed: 37614365
CCN1 interacts with integrins to regulate intestinal stem cell proliferation and differentiation [ Nat Commun, 2022, 13(1):3117]	PubMed: 35660741
Loss of non-motor kinesin KIF26A causes congenital brain malformations via dysregulated neuronal migration and axonal growth as well as apoptosis [ Dev Cell, 2022, 57(20):2381-2396.e13]	PubMed: 36228617

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。