VS-4718 (PND-1186)

Background Information:

The cytoplasmic tyrosine kinase FAK (Focal Adhesion Kinase) is a
signal transducer for integrins and is constitutively activated in
various tumor cell types. It is involved in tumor cell invasion,
migration and proliferation and plays a key role in the development,
function and survival of cancer stem cells (CSCs). VS-4718 (PND-1186) is
a potent, selective and orally bioavailable FAK inhibitor with IC50 at
low nM range. It blocks fibronectin-stimulated FAK autophosphorylation
of Tyr397, and prevents the integrin-mediated activation of several
downstream signal transduction pathways, including ERK, JNK/MAPK and
PI3K/Akt, resulting in the reduction of the number of cancer stem cells
and inhibition of tumor cell migration, proliferation and survival. It
displays strong anticancer activities both in vitro and in vivo, and is
currently in clinical evaluation.

Reference:

1. I. Tancioni, et al., FAK Inhibition disrupts a β5 integrin
signaling axis controlling anchorage-independent ovarian carcinoma
growth, Mol Cancer Ther. 2014 Aug;13(8):2050-61.
2. W. F. Tam, et al, VS-4718, a Potent Focal Adhesion Kinase (FAK)
Inhibitor, Exhibits Anticancer Activity in Leukemia Models in Vitro and
in Vivo.

APIM050257: VS-4718 (PND-1186)

CAS No.: 1061353-68-1.
Molecular Formula: C₂₅H₂₆F₃N₅O₃ • 0.8H₂O.
Molecular Weight: 515.9.
Purity: 99.9% (HPLC at 214 and 254 nm).
QC: HPLC-MS, ¹HNMR, Microanalysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.