1224887-10-8

Basic information

• Product Name: GSK-2256098
• Synonyms: GSK-2256098;2-(5-chloro-2-(1-isopropyl-3-methyl-1H-pyrazol-5-ylamino)pyridin-4-ylamino)-N-methoxybenzamide;GTPL7939;Benzamide, 2-[[5-chloro-2-[[3-methyl-1-(1-methylethyl)-1H-pyrazol-5-yl]amino]-4-pyridinyl]amino]-N-methoxy-
• CAS NO: 1224887-10-8
• Molecular Formula: C₂₀H₂₃ClN₆O₂
• Molecular Weight: 414.88862
• Product Categories: Inhibitors
• Mol File: 1224887-10-8.mol

Chemical Properties

• Appearance: /
• Density: 1.32±0.1 g/cm3(Predicted)
• PKA: 5.24±0.10(Predicted)
• CAS DataBase Reference: GSK-2256098(CAS DataBase Reference)
• NIST Chemistry Reference: GSK-2256098(1224887-10-8)
• EPA Substance Registry System: GSK-2256098(1224887-10-8)

Safety Data

• Hazardous Substances Data: 1224887-10-8(Hazardous Substances Data)

Usage

Uses

Used in Cancer Research and Treatment:
GSK-2256098 is used as a FAK inhibitor for targeting molecular pathways in cancer cells. It has been shown to inhibit FAK autophosphorylation at tyrosine 397 (Y397) in various cancer cell lines, such as OVCAR8 ovarian, U87MG glioblastoma, and A549 lung cancer cell lines. By inhibiting FAK, GSK-2256098 induces apoptosis, increases PARP levels, decreases cell viability, and inhibits colony formation in cancer cells.
Used in Biological Studies:
GSK-2256098 is used as a research tool for studying the role of FAK in various cellular processes, such as cell adhesion, migration, and survival. Its selective inhibition of FAK allows researchers to investigate the molecular mechanisms underlying these processes and identify potential therapeutic targets for cancer treatment.
Used in Drug Development:
GSK-2256098 serves as a lead compound for the development of new FAK inhibitors with improved potency, selectivity, and pharmacokinetic properties. These improved inhibitors can be used in the development of novel cancer therapies that target FAK-mediated signaling pathways, potentially leading to more effective treatments for various types of cancer.
Used in Preclinical Models:
GSK-2256098 is used in preclinical models, such as the Ishikawa orthotopic mouse model of uterine cancer, to evaluate its efficacy in reducing tumor weight and metastasis. These studies provide valuable insights into the potential therapeutic benefits of FAK inhibition in cancer treatment and help guide the design of future clinical trials.

Upstream product

• 1201935-41-2 2-[(2,5-dichloro-4-pyridinyl)amino]-N-(methyloxy)benzamide 
• 1124-16-9 3-methyl-1-(1-methylethyl)-1H-pyrazol-5-amine 
• 1224887-83-5 2-[(5-chloro-2-{[3-methyl-1-(1-methylethyl)-1H-pyrazol-5-yl]amino}-4-pyridinyl)amino]benzoic acid 
• 593-56-6 N-methoxylamine hydrochloride 
• 1224887-82-4 2-[(5-chloro-2-{[3-methyl-1-(1-methylethyl)-1H-pyrazol-5-yl]amino}-4-pyridinyl)a mino]benzonitrile 
• 1224887-80-2 2-[(2,5-dichloro-4-pyridinyl)amino]benzonitrile 
• 796851-03-1 2,5-dichloro-4-iodo-pyridine 
• 1885-29-6 anthranilic acid nitrile 

Relevant articles and documents

METHOD OF ADMINISTRATION AND TREATMENT

This invention relates to a method of treating cancer in a human in need thereof, comprising determining the presence or absence of a detectable amount of a gene product of the Neurofibromin-2 (NF2) gene in a sample from said human, and administering to said human an effective amount of a focal adhesion kinase (FAK) inhibitor, or a pharmaceutically acceptable salt thereof, if no gene product or no isoform 1 gene product is detected. This invention also relates to a method of treating cancer in a human in need thereof, comprising determining the presence or absence of a detectable amount of a functional isoform 1 protein of the NF2 gene, or a functional fragment thereof, in a sample from said human, and administering to said human an effective amount of a focal adhesion kinase (FAK) inhibitor, or a pharmaceutically acceptable salt thereof, if no gene product or no isoform 1 gene product is detected.

PYRAZOLYLAMINOPYRIDINES AS INHIBITORS OF FAK

The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R11, R12, R13, Q, Z, and p are as described herein. Compounds of the present invention are useful for the treatment of cancers.