A dose-dependent inhibitor of FAK

Defactinib – 1 mg

Brand:
Cayman
CAS:
1073154-85-4
Storage:
-20
UN-No:
Non-Hazardous - /

Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase that plays a vital role in many oncogenic pathways.{28867,28866} Defactinib is a dose-dependent inhibitor of FAK, with maximal inhibition of FAK autophosphorylation in cells achieved at 10 µM.{28865} It is less effective against the related kinase PYK2. Defactinib restores the chemosensitivity of taxane-resistant cells to paclitaxel (Item No. 10461), although it is not cytotoxic alone.{28865} Defactinib decreases YB-1 phosphorylation and nuclear accumulation in an Akt-dependent manner. It is orally bioavailable, inhibiting FAK and augmenting paclitaxel action in suppressing the growth and number of ovarian cancer cell tumors in mice.{28865}  

 

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Description

A dose-dependent inhibitor of FAK, with maximal inhibition of FAK autophosphorylation in cells achieved at 10 µM; restores the chemosensitivity of taxane-resistant cells to paclitaxel; orally bioavailable, inhibiting FAK and augmenting paclitaxel action against ovarian cancer cell tumors in mice

Formal name: N-​methyl-​4-​[[4-​[[[3-​[methyl(methylsulfon​yl)​amino]​-​2-​pyrazinyl]​methyl]​amino]​-​5-​(trifluoromethyl)​-​2-​pyrimidinyl]​amino]​-benzamide

Synonyms:  PF-04554878|VS-6063

Molecular weight: 510.5

CAS: 1073154-85-4

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 Signaling

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