GSK2256098
GSK2256098
CAS: 1224887-10-8
Molecular Formula: C20H23ClN6O2
GSK2256098 - Names and Identifiers
GSK2256098 - Physico-chemical Properties
| Molecular Formula | C20H23ClN6O2 |
| Molar Mass | 414.89 |
| Density | 1.32±0.1 g/cm3(Predicted) |
| Solubility | DMSO: ≥ 30 mg/mL |
| pKa | 5.24±0.10(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | GSK2256098 inhibits FAK activity by binding to tyrosine (Y) 397, the phosphorylation site of FAK. After the cancer cell lines OVCAR8 (ovary), U87MG (brain), and A549 (lung) were incubated with GSK2256098 for 30 minutes, GSK2256098 inhibited its FAK activity or Y397 phosphorylation, and the IC50 was 15, respectively, 8.5 and 12 nM. In addition, the intracellular inhibition of FAK by GSK2256098 appeared as early as 30 minutes after treatment and lasted for 12 hours in transplanted tumor mice. Inhibition of FAK activity by GSK2256098 resulted in a decrease in Akt and ERK activity. The PI3K/Akt and ERK signals are helpful for cell survival, so GSK2256098 can weaken some abnormal survival signaling pathways in some specific PDAC cells, which has medicinal value. GSK2256098 can promote the apoptosis of L3.6P1 through The caspase-9/PARP related pathway, and weaken the abnormal growth and abnormal migration ability of PDAC cells in a FAK specific manner. GSK2256098 can also inhibit the growth, migration, invasion and induce apoptosis of some GBM cell lines. |
| In vivo study | Pharmacokinetic tests in mice and rats showed that GSK2256098 had poor permeability into the central nervous system and could not effectively cross the blood-brain barrier. Then, it can reach a certain concentration in the tumor of patients with malignant glioma, accelerate the activity associated with preclinical tests. GSK2256098 has an acceptable safety profile, is effective at the target at or below the maximum tolerated concentration, and is clinically active in mesothelioma, especially in patients with merlin Moss. In the Ishikawa orthotoptopic mouse model, the treatment group of GSK2256098 had reduced tumor weight and tumor metastasis compared to the group of mice inoculated with Hec1A cells. In the treatment group, the density of tumor microvessels (CD31) was lower, the cell proliferation was less (Ki67), and the apoptosis rate was increased (TUNEL). GSK2256098 may have efficacy in uterine cancer patients with PTEN mutations, a potential predictive biomarker. |
GSK2256098 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.41 ml | 12.051 ml | 24.103 ml |
| 5 mM | 0.482 ml | 2.41 ml | 4.821 ml |
| 10 mM | 0.241 ml | 1.205 ml | 2.41 ml |
| 5 mM | 0.048 ml | 0.241 ml | 0.482 ml |
Last Update：2024-01-02 23:10:35
GSK2256098 - Reference Information
| biological activity | GSK2256098 is a potent, selective, reversible, ATP-competitive inhibitor of FAK kinase, the AP parent Ki was 0.4 nM. GSK2256098 can inhibit cancer cell growth and induce apoptosis. |
| Target | TargetValue FAK 0.4 nM(Ki) |
| Target | Value |
| FAK | 0.4 nM(Ki) |
| in vitro study | GSK2256098 inhibits FAK activity by binding to tyrosine (Y) 397, the phosphorylation site of FAK. After the cancer cell lines OVCAR8 (ovary), U87MG (brain), and A549 (lung) were incubated with GSK2256098 for 30 minutes, GSK2256098 inhibited its FAK activity or Y397 phosphorylation, and the IC50 was 15, respectively, 8.5 and 12 nM. In addition, the intracellular inhibition of FAK by GSK2256098 appeared as early as 30 minutes after treatment and lasted for 12 hours in transplanted tumor mice. Inhibition of FAK activity by GSK2256098 resulted in a decrease in Akt and ERK activity. The PI3K/Akt and ERK signals are helpful for cell survival, so GSK2256098 can weaken some abnormal survival signaling pathways in some specific PDAC cells, which has medicinal value. GSK2256098 can promote the apoptosis of L3.6P1 through The caspase-9/PARP related pathway, and weaken the abnormal growth and abnormal migration ability of PDAC cells in a FAK specific manner. GSK2256098 can also inhibit the growth, migration, invasion and induce apoptosis of some GBM cell lines. |
| in vivo studies | pharmacokinetic studies in mice and rats showed that GSK2256098 had poor permeability into the central nervous system, unable to effectively cross the blood-brain barrier. Then, it can reach a certain concentration in the tumor of patients with malignant glioma, accelerate the activity associated with preclinical tests. GSK2256098 has an acceptable safety profile, is effective at the target at or below the maximum tolerated concentration, and is clinically active in mesothelioma, especially in patients with merlin Moss. In the Ishikawa orthotoptopic mouse model, the treatment group of GSK2256098 had reduced tumor weight and tumor metastasis compared to the group of mice inoculated with Hec1A cells. In the treatment group, the density of tumor microvessels (CD31) was lower, the cell proliferation was less (Ki67), and the apoptosis rate was increased (TUNEL). GSK2256098 may have efficacy in uterine cancer patients with PTEN mutations, a potential predictive biomarker. |
Last Update：2024-04-09 20:52:54
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CAS: 1224887-10-8
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CAS: 1224887-10-8
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Product Name: GSK2256098 Visit Supplier Webpage Request for quotation
CAS: 1224887-10-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1224887-10-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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