PND-1186


CAS No. : 1061353-68-1

PND-1186,1061353-68-1
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000311
Synonyms:2-((2-((2-methoxy-4-morpholinophenyl)amino)-5-(trifluoromethyl)pyridin-4-yl)amino)-N-methylbenzamide
Molecular Formula:C₂₅H₂₆F₃N₅O₃
Molecular Weight:501.5
Target:FAK
IC50:1.5 nM [1]
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Appearance:Off-white to grey solid powder
Purity: > 98%
Cat No:I000311
Cas No:1061353-68-1
Product-Name:PND-1186
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
SMILES:CNC(=O)C1=CC=CC=C1NC2=CC(=NC=C2C(F)(F)F)NC3=C(C=C(C=C3)N4CCOCC4)OC

PND-1186 is a potent FAK inhibitor with IC50 of 1.5 nM.
IC50 Value: 1.5 nM [1]
Target: FAK
in vitro: PND-1186 has an IC50 of ~100 nM in breast carcinoma cells as determined by anti-phospho-specific immunoblotting to FAK Tyr-397. PND-1186 did not alter c Src or p130Cas tyrosine phosphorylation in adherent cells, yet functioned to restrain cell movement. Notably, 1.0 M 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 M PND-1186 blocked FAK and p130Cas tyrosine phosphorylation, promoted caspase-3 activation, and triggered cell apoptosis [1].
in vivo: Addition of PND-1186 to the drinking water of mice was well tolerated and inhibited ascites- and peritoneal membrane-associated ovarian carcinoma tumor growth associated with the inhibition of FAK Tyr-397 phosphorylation [1]. PND-1186 (100 mg/kg intraperitoneal, i.p.) showed promising pharmacokinetics (PK) and inhibited tumor FAK Tyr-397 phosphorylation for 12 hours. Oral administration of 150 mg/kg PND-1186 gave a more sustained PK profile verses i.p., and when given twice daily, PND-1186 significantly inhibited sygeneic murine 4T1 orthotopic breast carcinoma tumor growth and spontaneous metastasis to lungs [2].
Clinical trial: Phase I, Dose-Escalation Study of VS-4718 in Subjects With Metastatic Non-Hematological Malignancies. Phase 1


1:PND-1186 FAK inhibitor selectively promotes tumor cell apoptosis in three-dimensional environments. Schaller MD, Frisch SM.Cancer Biol Ther. 2010 May 15;9(10):791-3. Epub 2010 May 8. No abstract available. PMID: 20364110
2:Oral delivery of PND-1186 FAK inhibitor decreases tumor growth and spontaneous breast to lung metastasis in pre-clinical models. Walsh C, Tanjoni I, Uryu S, Tomar A, Nam JO, Luo H, Phillips A, Patel N, Kwok C, McMahon G, Stupack DG, Schlaepfer DD.Cancer Biol Ther. 2010 May 15;9(10):778-90. PMID: 20234193 Free PMC Article
3:PND-1186 FAK inhibitor selectively promotes tumor cell apoptosis in three-dimensional environments. Tanjoni I, Walsh C, Uryu S, Tomar A, Nam JO, Mielgo A, Lim ST, Liang C, Koenig M, Sun C, Patel N, Kwok C, McMahon G, Stupack DG, Schlaepfer DD.Cancer Biol Ther. 2010 May 15;9(10):764-77. PMID: 20234191 Free PMC Article
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