A FAK inhibitor; selective for FAK over 261 kinases; inhibits FAK autophosphorylation at Y397 in OVCAR8 ovarian

GSK2256098 – 1 mg

Brand:
Cayman
CAS:
1224887-10-8
Storage:
-20
UN-No:
Non-Hazardous - /

GSK2256098 is an inhibitor of focal adhesion kinase (FAK).{42043} It is selective for FAK, inhibiting only FAK greater than 50% in a panel of 261 kinases. GSK2256098 inhibits FAK autophosphorylation at tyrosine 397 (Y397) in OVCAR8 ovarian, U87MG glioblastoma, and A549 lung cancer cell lines (IC50s = 15, 8.5, and 12 nM, respectively). It induces apoptosis and increases PARP levels, decreases viability (IC50 = 25 µM), and inhibits colony formation in L3.6P1 cells. GSK2256098 (75 mg/kg per day) also leads to lower tumor weight and fewer metastases in the Ishikawa orthotopic mouse model of uterine cancer.{42044}  

 

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SKU: 22955 - 1 mg Category:

Description

A FAK inhibitor; selective for FAK over 261 kinases; inhibits FAK autophosphorylation at Y397 in OVCAR8 ovarian, U87MG glioblastoma, and A549 lung cancer cell lines (IC50s = 15, 8.5, and 12 nM, respectively); induces apoptosis, decreases viability (IC50 = 25 µM), and inhibits colony formation in L3.6P1 cells; leads to lower tumor weight and fewer metastases in an orthotopic mouse model of uterine cancer at 75 mg/kg per day

Formal name: 2-[[5-chloro-2-[[3-methyl-1-(1-methylethyl)-1H-pyrazol-5-yl]amino]-4-pyridinyl]amino]-N-methoxy-benzamide

Synonyms: 

Molecular weight: 414.9

CAS: 1224887-10-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Non-Receptor Tyrosine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling

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