General description

A cell-permeable imidazopyridine compound that acts as a highly potent and ATP-competitive DNA-PK and p110α-selective PI3-K inhibitor (IC₅₀ = 0.3, 40, 100, and 850 nM for p110α, p110γ, PI 3-K C2β, and p110β, respectively). Shown to effectively block cellular PI3-K/Akt signaling and inhibit tumor growth both in vitro (IC₅₀ ≤58 nM in MCF7, MCF7 ADR-res, HeLa, A375, and A549 cultures) and in mice in vivo (62% inhibition of HeLa xenograft in 2 weeks, 50 mg/kg/day, i.p.).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Kim, S., et al. 2007. Blood110, 4206. Hayakawa, M., et al. 2007. Bioorg. Med. Chem.15, 5837. Knight, Z.A., et al. 2007. Cell125, 733.

Packaging

Packaged under inert gas

5 mg in Plastic Bag(s)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Regulatory Review (Z)