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Defactinib

Defactinib Structural

What is Defactinib?

Description

Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase that plays a vital role in many oncogenic pathways. Defactinib is a dose-dependent inhibitor of FAK, with maximal inhibition of FAK autophosphorylation in cells achieved at 10 μM. It is less effective against the related kinase PYK2. Defactinib restores the chemosensitivity of taxane-resistant cells to paclitaxel , although it is not cytotoxic alone. 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.

The Uses of Defactinib

Defactinib is a selective and orally active FAK inhibitor phase 2. Used in treating cancer patients as it decreases proliferation and increases apoptosis.

storage

Store at -20°C

References

1) Jones?et al.?(2015),?A phase I study of VS-6063, a second-generation focal adhesion kinase inhibitor, in patients with advanced solid tumors;?Invest. New Drugs?33?1100 2) Kolev?et al.?(2017),?Inhibition of FAK kinase activity preferentially targets cancer stem cells;?Oncotarget?8?51733 3) Marcucci?et al.?(2016),?Anti-Cancer Stem-like Cell Compounds in Clinical Development – An Overview and Critical Appraisal;?Front. Oncol.?6?115 4) Ring?et al.?(2015),?FAK/PYK2 inhibitors defactinib and VS-4718 enhance immune checkpoint inhibitor efficacy;?J. Immunother. Cancer?3?354 5) NCT02546531 6) Jiang?et al.?(2016),?Targeting Focal Adhesion Kinase Renders Pancreatic Cancers Responsive to Checkpoint Immunotherapy;?Nat. Med.?22?851

Properties of Defactinib

Density  1.495±0.06 g/cm3(Predicted)
storage temp.  -20°C (des.)
solubility  Soluble in DMSO (up to at least 25mg/ml)
form  solid
pka 15.16±0.46(Predicted)
color  White
Stability: Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

Safety information for Defactinib

Computed Descriptors for Defactinib

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