Chemdea |
PIK-75 – PI3Ka Inhibitor VIII |
Catalog # CD0273 |
Price: 1 mg - $10;
5 mg - $15; 10 mg - $28; 25 mg - $54; 50 mg - $95; 100 mg - $162; 200 mg -
$316; 1 g- $1425 |
Availability: In stock |
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. PACKAGED UNDER INERT GAS. Purity: 99% by HPLC. CAS # 372196-67-3. Solubility: DMSO (10 mg/mL). Molecular Formula: C16H14N5O4SBr•HCl•2H2O. Molecular Weight: 524.8.
A cell-permeable
imidazopyridine compound that acts as a highly potent and ATP-competitive
DNA-PK and p110α-selective PI3-K inhibitor (IC50 = 7.8, 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.).
Reference: 1. Hayakawa, M. et al. Bioorg. Med. Chem. Letters. 2007, 15, 5837; 2. Knight, Z. A. et al. Cell 2006, 125, 733; 3. Chaussade C. et al. Biochem J. 2007, 404, 449; 4. Kim S. et al. Blood, 2007, 110, 4206. |
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