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Products > Protein Tyrosine Kinase/RTK > FAK > GSK2256098
Product name : GSK2256098
Item : C2461
Price : 200mg, $750;500mg, $1290; 1g, $1990; 2g, $2995
contact : Send inquiry to: info@acesobio.com
CAS : 1224887-10-8
Molecular Weight : 414.89
Formula : C20H23ClN6O2
Storage : at -20°C
Additional information : We offer significant discount for bulky quantity order.
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Details:
Description of:GSK2256098(CAS:1224887-10-8)
GSK2256098, also known as GTPL7939, is a focal adhesion kinase-1 (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. FAK inhibitor GSK2256098 inhibits FAK, which may prevent the integrin-mediated activation of several downstream signal transduction pathways, including ERK, JNK/MAPK and PI3K/Akt, thereby inhibiting tumor cell migration, proliferation and survival, and tumor angiogenesis. The tyrosine kinase FAK is normally activated by binding to integrins in the extracellular matrix (ECM) but may be upregulated and constitutively activated in various tumor cell types.
GSK2256098 is a thousand fold more selective for FAK compared to the nearest FAK family member, Pyk2. GSK2256098 inhibits FAK activity through targeting the phosphorylation site of FAK, tyrosine (Y) 397. GSK2256098 inhibits FAK activity or Y397 phosphorylation in cancer cell lines, OVCAR8 (ovary), U87MG (brain), and A549 (lung), at IC50s of 15, 8.5 and 12 nM, respectively. The responses of 6 PDAC cell lines in regards to FAK Y397 phosphorylation or activity to GSK2256098 treatments (0.1–10 μM) ranged from low (less than 20% inhibition) to high (more than 90% inhibition). The least and most sensitive cell lines (PANC-1 and L3.6P1) are selected for further analysis. GSK2256098 inhibition of FAK Y397 phosphorylation correlated with decreased levels of phosphorylated Akt and ERK in L3.6P1 cells. GSK2256098 decreases cell viability, anchorage-independent growth, and motility in a dose dependent manner

Quality control data:
Quality control by 1H-NMR, 13C-NMR, HPLC and LCMS.
Product will be shipped with supporting analytical data.

REFERENCES

 1: Thanapprapasr D, Previs RA, Hu W, Ivan C, Armaiz-Pena GN, Dorniak PL, Hansen 
JM, Rupaimoole R, Huang J, Dalton HJ, Ali-Fehmi R, Coleman RL, Sood AK. PTEN 
Expression as a Predictor of Response to Focal Adhesion Kinase Inhibition in 
Uterine Cancer. Mol Cancer Ther. 2015 Jun;14(6):1466-75. doi: 
10.1158/1535-7163.MCT-14-1077. Epub 2015 Apr 1. PubMed PMID: 25833835; PubMed 
Central PMCID: PMC4458384.

2: Zhang J, He DH, Zajac-Kaye M, Hochwald SN. A small molecule FAK kinase 
inhibitor, GSK2256098, inhibits growth and survival of pancreatic ductal 
adenocarcinoma cells. Cell Cycle. 2014;13(19):3143-9. doi: 
10.4161/15384101.2014.949550. PubMed PMID: 25486573; PubMed Central PMCID: 
PMC4615113.

3: Schultze A, Fiedler W. Clinical importance and potential use of small molecule 
inhibitors of focal adhesion kinase. Anticancer Agents Med Chem. 2011 
Sep;11(7):593-9. Review. PubMed PMID: 21787277.

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