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Description: Potent FAK inhibitor; orally bioavailable
Chemical Name: 2-[[2-[[2-Methoxy-4-(4-morpholinyl)phenyl]amino]-5-(trifluoromethyl)-4-pyridinyl]amino]-N-methylbenzamide
Purity: ≥98% (HPLC)
Biological Activity for PND 1186
PND 1186 is a potent FAK inhibitor (IC50 values are 1.5 and 100 nM for recombinant FAK and FAK in breast carcinoma cells, respectively). Promotes caspase activation; triggering apoptosis. Inhibits 4T1 breast carcinoma subcutaneous tumor growth and breast carcinoma cell motility. Decreases spontaneous breast to lung metastasis in pre-clinical models. Orally bioavailable.
Compound Libraries for PND 1186
PND 1186 is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for PND 1186
| M. Wt | 501.51 |
| Formula | C25H26F3N5O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1061353-68-1 |
| PubChem ID | 25073775 |
| InChI Key | IGUBBWJDMLCRIK-UHFFFAOYSA-N |
| Smiles | CNC(=O)C1=C(NC2=CC(NC3=C(OC)C=C(C=C3)N3CCOCC3)=NC=C2C(F)(F)F)C=CC=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for PND 1186
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 50.15 | 100 |
Preparing Stock Solutions for PND 1186
The following data is based on the product molecular weight 501.51. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.99 mL | 9.97 mL | 19.94 mL |
| 5 mM | 0.4 mL | 1.99 mL | 3.99 mL |
| 10 mM | 0.2 mL | 1 mL | 1.99 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
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Product Datasheets for PND 1186
References for PND 1186
References are publications that support the biological activity of the product.
Walsh et al (2010) Oral delivery of PND-1186 FAK inhibitor decreases tumor growth and spontaneous breast to lung metastasis in pre-clinical models. Cancer Biol.Ther. 9 778 PMID: 20234193
Tanjoni et al (2010) PND-1186 FAK inhibitor selectively promotes tumor cell apoptosis in three-dimensional environments. Cancer Biol.Ther. 9 764 PMID: 20234191
Jiang et al (2016) Targeting focal adhesion kinase renders pancreatic cancers responsive to checkpoint immunotherapy. Nat.Med. 22 851 PMID: 27376576
If you know of a relevant reference for PND 1186, please let us know.
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Keywords: PND 1186, PND 1186 supplier, PND1186, SR2516, VS4718, SR_2516, VS_4718, potent, FAK, inhibitors, inhibits, orally, bioavailable, caspase, activators, Focal, Adhesion, Kinase, 6891, Tocris Bioscience
Citations for PND 1186
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