N-((1E)-(6-Bromoimidazo[1,2-a]pyridin-3-yl)methylene)-N′-methyl-N′′-(2-methyl-5-nitrobenzene)sulfonohydrazide, HCl Pale yellow solid. PROTECT FROM LIGHT. HYGROSCOPIC. PACKAGED UNDER INERT GAS. A cell-permeable imidazopyridine compound that acts as a highly potent and ATP-competitive DNA-PK and p110a-selective PI3-K inhibitor (IC50 = 0.3, 40, 100, and 850 nM for p110a, p110g, PI 3-K C2b, and p110b, 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.). Purity: ≥95% by HPLC. Ref.: Kim, S., et al. 2007. Blood 110, 4206. Hayakawa, M., et al. 2007. Bioorg. Med. Chem. 15, 5837. Knight, Z.A., et al. 2007. Cell 125, 733. |
