PND 1186

Pricing Availability   Qty
Cat.No. 6891 - PND 1186 | C25H26F3N5O3 | CAS No. 1061353-68-1
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)
Datasheet
Citations
Reviews
Literature

Biological Activity

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.

Technical Data

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 50.15 100

Preparing Stock Solutions

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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References

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


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Citations for PND 1186

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