Apoptosis
Telomerase
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Product name : NVP-BAG956
Item : cc502
Price : 200mg, $1250;500mg, $2150; 1g $3050; 2g, $4450
contact : Send inquiry to: info@acesobio.com,or by fax to: 1-845-673-1239.
CAS : 853910-02-8
Molecular Weight : 427.5
Formula : C₂₈H₂₁N₅
Storage : at -20°C
Additional information : We offer significant discount for larger quantity order
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NVP-BAG956 is a cell-permeable imidazoquinoline compound that acts as a potent, reversible, and ATP-competitive PI 3-K/PDK1 dual kinase inhibitor (IC50 = 56, 446, 35, 117, and 245 nM against p110α, p110β, p110δ, p110γ, and PDK1, respectively), displaying much reduced potency against VEGFR1 (IC50 = 2.56 µM) and little or no activity toward a panel of 15 other kinases (IC50 >10 µM). Shown to effectively inhibit the constitutive phosphorylation of PKB (T308 & S473; IC50 ≤45 nM) as well as PKB downstream effectors GSK3β (S9), FKHRL1 (T32), and p70S6K (T389) in human glioma U87MG and adeonocarcinoma PC3M cultures with PTEN deletion in vitro and retard PC3M-derived tumor growth in mice (by 50%; 75 mg/kg; twice per day p.o.) in vivo. Also reported to exhibit antiproliferative activities against BCRF-ABL- and mutant FLT3-expressing cells either alone or in combination with other PI3K/AKT, mTOR, and tyrosine kinase inhibitors. [1][2]
Reference:
[1] Blood 2008, 111, 3723-3734.J Biol. Chem. 2006, 280, 19867-19874.
[2] Bioorg. Med. Chem. Lett. 2008, 18, 1027-1030.
Chemical Information
PLEASE KEEP THE PRODUCT UNDER -20℃ FOR LONG-TERM STORAGE.
NOT FOR HUMAN OR VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.
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