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PND 1186
- SR 2516 - VS 4718
Axon 2459
CAS:
1061353-68-1
Purity:
100%
- Soluble in DMSO
- MF: C25H26F3N5O3
- MW: 501.5
Description
PND 1186 (VS-4718) is an orally active dual inhibitor of focal adhesion kinase (FAK/PTK2) and PYK2. It suppresses FAK/p130Cas phosphorylation and promotes apoptosis in tumor-cell models.
FAK and PYK2 integrate integrin, growth-factor and microenvironmental signals controlling adhesion, migration, survival and tumor invasion. PND 1186 is useful for studying focal adhesion signaling, metastasis biology and tumor-stroma interactions.
Key Features
- Dual FAK/PYK2 kinase inhibitor
- Reported in vitro IC50: 1.5 nM for FAK
- Blocks FAK and p130Cas tyrosine phosphorylation
- Promotes caspase-3 activation and tumor-cell apoptosis in reported models
Applications
- FAK/PYK2 signaling research
- Cancer cell migration and invasion assays
- Tumor microenvironment pharmacology
- Integrin and focal adhesion pathway studies
More Information
| Parent CAS No. | 1061353-68-1 |
|---|---|
| Chemical Name | 2-(2-(2-methoxy-4-morpholinophenylamino)-5-(trifluoromethyl)pyridin-4-ylamino)-N-methylbenzamide |
| SMILES | C(NC)(=O)C1=CC=CC=C1NC1C(C(F)(F)F)=CN=C(NC2=CC=C(N3CCOCC3)C=C2OC)C=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C25H26F3N5O3/c1-29-24(34)17-5-3-4-6-19(17)31-21-14-23(30-15-18(21)25(26,27)28)32-20-8-7-16(13-22(20)35-2)33-9-11-36-12-10-33/h3-8,13-15H,9-12H2,1-2H3,(H,29,34)(H2,30,31,32) |
| InChiKey | IGUBBWJDMLCRIK-UHFFFAOYSA-N |
| CID | 25073775 |
| Short Description | FAK/PYK2 inhibitor |
References
- I. Tanjoni et al. PND-1186 FAK inhibitor selectively promotes tumor cell apoptosis in three-dimensional environments. Cancer Biol Ther. 2010 May 15;9(10):764-77.
- C. Walsh et al. Oral delivery of PND-1186 FAK inhibitor decreases tumor growth and spontaneous breast to lung metastasis in pre-clinical models. Cancer Biol Ther. 2010 May 15;9(10):778-90.
- Y. Zhang et al. Pyk2 promotes tumor progression in multiple myeloma. Blood. 2014 Oct 23;124(17):2675-86.
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