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PDK1 inhibitor 2610
- Parent CAS: 853909-77-0
- Soluble in water and DMSO
- MF: C25H15N5.HCl
- MW: 421.88
Description
PDK1 inhibitor 2610 (Axon 2610) is a potent, ATP-competitive and selective dual PI3K/PDK1 inhibitor. It exhibits strong inhibition with an IC50 of 34 nM against PDK1. It subsequently blocks p-T308-PKB (Akt) phosphorylation with an IC50 of 94 nM. It also inhibits four isoforms of PI3K with IC50 values of 64 nM, 432 nM, 98 nM, and 67 nM for p110α, p110β, p110δ, and p110γ, respectively.
PI3K/PDK1 pharmacology is central to oncology, as the PI3K/PDK1 signaling pathway acts as a a master regulator of cell survival, growth, and metabolism. PDK1 inhibitor 2610 supports mechanistic studies of PDK1, PI3K and dual PI3K/PDK1 inhibition across biochemical, cellular and disease-model assays.
Key Features
- Potent and ATP-competitive PI3K/PDK1 inhibitor
- IC50 values of 34 nM against PDK1 and 64 nM, 432 nM, 98 nM, and 67 nM against PI3k p110α, p110β, p110δ, and p110γ, respectively
- Selective dual inhibition of PDK1 and the upstream PI3K signaling pathway
- Probe to modulate P3K/PDK1-dependent signaling or biological activity
Applications
- PI3K/PDK1 pharmacology and target-validation studies
- PI3K/PDK1 pathway and signaling assays
- Disease-model research related to oncology
- Kinase signaling, phosphorylation and pathway-inhibition assays
Note: Axon 2610 is a close analogue of NVP-BAG956 (Axon 1282)
More Information
| Parent CAS No. | 853909-77-0 |
|---|---|
| Chemical Name | 2-(4-(8-(pyridin-3-ylethynyl)-1H-imidazo[4,5-c]quinolin-1-yl)phenyl)acetonitrile hydrochloride |
| SMILES | C1(CC#N)=CC=C(N2C3C4C(N=CC=3N=C2)=CC=C(C#CC2=CC=CN=C2)C=4)C=C1.Cl |
| MFCD | N.A. |
| 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 |
| InChiKey | RUXNLVOZJZTQAS-UHFFFAOYSA-N |
| CID | 122129988 |
| Short Description | PI3K/PDK1 inhibitor |
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