WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406262
Description: PND-1186, also known as SR-2156 and VS-4718, is a potent FAK inhibitor with a 50% inhibitory concentration (IC50) of 1.5 nM in vitro. PND-1186 has an IC50 of ~100 nM in breast carcinoma cells. Notably, 1.0 ÂµM PND-1186 (>5-fold above IC50) had limited effects on cell proliferation. However, under non-adherent conditions as spheroids and as colonies in soft agar, 0.1 ÂµM PND-1186 blocked FAK and p130Cas tyrosine phosphorylation, promoted caspase-3 activation, and triggered cell apoptosis. PND-1186 inhibited 4T1 breast carcinoma subcutaneous tumor growth correlated with elevated tumor cell apoptosis and caspase 3 activation.
MedKoo Cat#: 406262
Chemical Formula: C25H26F3N5O3
Exact Mass: 501.19877
Molecular Weight: 501.5
Elemental Analysis: C, 59.87; H, 5.23; F, 11.36; N, 13.96; O, 9.57
Synonym: PND1186; PND 1186; PND1186; SR 2516; SR2516; SR2516; VS4718; VS4718; VS 4718.
IUPAC/Chemical Name: 2-((2-((2-methoxy-4-morpholinophenyl)amino)-5-(trifluoromethyl)pyridin-4-yl)amino)-N-methylbenzamide.
SMILES Code: O=C(NC)C1=CC=CC=C1NC2=CC(NC3=C(OC)C=C(N4CCOCC4)C=C3)=NC=C2C(F)(F)F
1: Tancioni I, Uryu S, Sulzmaier FJ, Shah NR, Lawson C, Miller NL, Jean C, Chen XL, Ward KK, Schlaepfer DD. FAK Inhibition disrupts a β5 integrin signaling axis controlling anchorage-independent ovarian carcinoma growth. Mol Cancer Ther. 2014 Aug;13(8):2050-61. doi: 10.1158/1535-7163.MCT-13-1063. Epub 2014 Jun 4. PubMed PMID: 24899686; PubMed Central PMCID: PMC4126870.