Saturday, August 24, 2013

FAK INHIBITORS ARE HERE AS A MATTER OF FACT!

Verastem Enters Biomarker Agreement with LabCorp for Cancer Stem Cell Agent Companion Diagnostic




:The identification of patients most likely to benefit from targeted therapy is critical to accelerating the drug development and approval process,” said Henri Termeer, Verastem Lead Director.
Clinical assay validation is an integral component to all companion diagnostics entering an FDA approval process.
Pioneering research by Robert Weinberg, Ph.D., Verastem cofounder and chair of the Scientific Advisory Board, and others have demonstrated that FAK signaling plays a central role in the tumor-initiating capability of cancer stem cells and ultimate disease progression. VS-6063 is designed to target and kill cancer stem cells by inhibiting FAK signaling.
Mesothelioma tumors lacking the tumor suppressor Merlin appear to be particularly sensitive to FAK inhibitors. As shown recently at the EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics, sensitivity due to lack of Merlin is evident in both research models and early clinical proof-of-concept.
“We believe the approximately 50% of mesothelioma patients lacking Merlin may be particularly responsive to treatment with FAK inhibitors,” said Dan Paterson, Verastem Vice President, Head of Corporate Development and Diagnostics. “LabCorp is the perfect partner to progress our research on Merlin into a companion diagnostic for VS-6063.”"
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 SANTA CRUZ BIOTECHNOLOGY
FAK Inhibitor 14 is a selective FAK (focal adhesion kinase) inhibitor that displays no significant activity for a range of other kinases including PDGFR, EGFR, and IGF-RI. FAK Inhibitor 14 has been shown to prevent FAK autophosphorylation at the putative activation site, tyrosine 397 (IC50 of 1μM). FAK Inhibitor 14 has been shown to promote cell detachment and inhibit cell adhesion in vitro, and to exhibit antiproliferative activity in a variety of human tumor cell lines in vivo such as: breast cancer cell lines BT474 and MCF-7, pancreatic cancer cell lines Panc-1 and Miapaca-2, and neuroblastoma cell lines MYCN+/MYCN- (with a greater effect on the negative isogenic form). FAK Inhibitor 14 has also been used to study the conformation and self replication methodology of bis capped porphyrins.
Technical Information
Appearance:Gray solid
Physical State:Solid
Solubility:Soluble to 100 mM in Water and to 75 mM in DMSO
Melting Point:>300 °C lit.
Safety and Reference Information
PubChem CID:78260
MDL Number:MFCD00012970
EC Number:224-822-6
SMILES:C1=C(C(=CC(=C1N)N)N)N.Cl.Cl.Cl.Cl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
References
1. Thordarson, P., et al. 2003. Org. Biomol. Chem. 1: 1216-1225. PMID: 12926398
2. Golubovskaya, V.M., et al. 2008. J. Med. Chem. 51: 7405-7416. PMID: 18989950
3. Hochwald, S.N., et al. 2009. Cell Cycle. 8: 2435-2443. PMID: 19571674
4. Beierle, E.A., et al. 2010. Cell Cycle. 9: 1005-1015. PMID: 20160475

FAK Inhibitor 14 (CAS 4506-66-5) Product Citations
See how others have used FAK Inhibitor 14 (CAS 4506-66-5).


3 total citations
Bartolomé RA. et al. 2013. Cadherin-17 interacts with α2β1 integrin to regulate cell proliferation and adhesion in colorectal cancer cells causing liver metastasis. Oncogene. : . View PubMed Entry
Marley, K. et al. 2012. Phosphotyrosine enrichment identifies focal adhesion kinase and other tyrosine kinases for targeting in canine hemangiosarcoma. Vet Comp Oncol. 10: 214-222. View PubMed Entry
Park, JA. et al. 2010. The chitinase-like protein YKL-40 is secreted by airway epithelial cells at baseline and in response to compressive mechanical stress. J Biol Chem. : -. View PubMed Entry
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 GIVEN THE NON SPECIFICITY OF THESE BIOMAKERS, I SUSPECT THESE INHIBITORS WILL HAVE A ROLE IN MAINTENANCE AND PREVENTION SETTING UNLESS IT IS ASSUMED THERE IS A DRIVER MUTATION HIDDEN IN THIS PATHWAY!
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