A reversible inhibitor of both Aurora A and B kinases (IC50s = 0.8 and 5 nM

PF-03814735 – 5 mg

Brand:
Cayman
CAS:
942487-16-3
Storage:
-20
UN-No:
Non-Hazardous - /

The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. PF-03814735 is a reversible inhibitor of both Aurora A and B kinases with IC50 values of 0.8 and 5 nM, respectively, in in vitro activity assays.{22524} PF-03814735 also inhibits the kinases FLT1, FAK, TrkA, Met, and FGFR1 with IC50 values of 10, 22, 30, 100, and 100 nM, respectively.{22524} PF-03814735 inhibits cell proliferation of HCT116, HL-60, A549, and H125 tumor cell lines with IC50 values ranging from 42-150 nM and shows in vivo efficacy in an HCT116 tumor xenograft mouse model.{22524} PF-03814735 has been shown to be particularly sensitive towards inhibiting the growth of small cell lung cancer cell lines and other tumors driven by the Myc family genes.{22525}  

 

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Description

A reversible inhibitor of both Aurora A and B kinases (IC50s = 0.8 and 5 nM, respectively); also inhibits FLT1, FAK, TrkA, Met, and FGFR1 (IC50s = 10, 22, 30, 100, and 100 nM, respectively)

Formal name: N-[2-[(1S,4R)-6-[[4-(cyclobutylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1,2,3,4-tetrahydronaphthalen-1,4-imin-9-yl]-2-oxoethyl]-acetamide

Synonyms: 

Molecular weight: 474.5

CAS: 942487-16-3

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Aurora||Product Type|Biochemicals|Kinase Inhibitors|FGFR Family||Product Type|Biochemicals|Kinase Inhibitors|Other Non-Receptor Tyrosine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|ATM Signaling||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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