| Bioactivity | GSK2256098 is a selective FAK kinase inhibitor, which inhibits growth and survival of pancreatic ductal adenocarcinoma cells. | ||||||||||||
| Invitro | 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[1]. | ||||||||||||
| Name | GSK2256098 | ||||||||||||
| CAS | 1224887-10-8 | ||||||||||||
| Formula | C20H23ClN6O2 | ||||||||||||
| Molar Mass | 414.89 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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GSK2256098
CAS: 1224887-10-8 F: C20H23ClN6O2 W: 414.89
GSK2256098 is a selective FAK kinase inhibitor, which inhibits growth and survival of pancreatic ductal adenocarcinoma c
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