PND-1186

• CAT Number: I000311
• CAS Number: 1061353-68-1
• Molecular Formula: C25H26F3N5O3
• Molecular Weight: 501.5
• Purity: ≥95%
• Target: FAK
• Solubility: DMSO: ≥ 34 mg/mL
• Storage: Store at -20°C
• IC50: 1.5 nM
• IUPAC Name: 2-[[2-(2-methoxy-4-morpholin-4-ylanilino)-5-(trifluoromethyl)pyridin-4-yl]amino]-N-methylbenzamide
• 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 (CAT: I000311) is a potent FAK (focal adhesion kinase) inhibitor that has been developed as an anti-tumor drug for cancer therapy. In vitro studies have shown that PND-1186 inhibits FAK phosphorylation, leading to the inhibition of cell movement and the promotion of cell apoptosis in breast carcinoma cells. It has demonstrated limited effects on cell proliferation but has shown efficacy in blocking tumor growth and metastasis in vivo. PND-1186 has been well-tolerated in preclinical studies, and clinical trials are being conducted to evaluate its safety and efficacy in patients with metastatic non-hematological malignancies.

Overview of Clinical Research

PND-1186 is under investigation in clinical trial NCT02215629 (Dose Escalation Study in Acute Myeloid or B-Cell Acute Lymphoblastic Leukemia).

Reference

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