PDK1 inhibitor 2610

• CAT Number: I047616
• CAS Number: 2108463-93-8
• Molecular Formula: C25H15N5.HCl
• Molecular Weight: 421.88
• Purity: ≥95%
• IUPAC Name: 2-[4-[8-(2-pyridin-3-ylethynyl)imidazo[4,5-c]quinolin-1-yl]phenyl]acetonitrile;hydrochloride
• InChI: InChI=1S/C25H15N5.ClH/c26-12-11-18-5-8-21(9-6-18)30-17-29-24-16-28-23-10-7-19(14-22(23)25(24)30)3-4-20-2-1-13-27-15-20;/h1-2,5-10,13-17H,11H2;1H
• SMILES: C1=CC(=CN=C1)C#CC2=CC3=C4C(=CN=C3C=C2)N=CN4C5=CC=C(C=C5)CC#N.Cl

Potent, ATP-competitive and selective dual PI3K and PDPK1 inhibitor (IC50 values 34 nM and 94 nM for PDK1 and p-T308-PKB inhibition, respectively. Also inhibits PI3K p110α, p110β, p110δ, and p110γ (IC50 values 64 nM, 432 nM , 98 nM, and 67 nM, respectively).
Axon 2610 is a close analogue of NVP-BAG956 (Axon 1282)
KEYWORDS: PDK1 inhibitor 2610 | supplier | PI3K/PDK1 inhibitor | CAS [2108463-93-8],[853909-77-0] | Phosphatidylinositol | PI3K | PDPK | Inhibitor | PKB | Akt | p110 | Oncology | PIP3 | Novartis

Reference

F Stauffer et al. Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1027-30.

 

ST  Murphy et al. Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1). J Med Chem. 2011 Dec 22;54(24):8490-500.