NVP-BAG956 inhibits cellular AKT phosphorylation at Thr308.NVP-BAG956 displayed the most powerful cytotoxic affects against T-ALL cell lines and primary patients samples, when compared with a pan class I PI3K inhibitor (GDC-0941), an allosteric Akt inhibitor (MK-2206), an mTORC1 allosteric inhibitor (RAD-001), or an ATP-competitive mTORC1/mTORC2 inhibitor (KU63794).BAG956 blocks AKT phosphorylation induced by BCR-ABL-, and induce apoptosis of BCR-ABL-expressing cell lines and patient bone marrow cells at concentrations that also inhibit PI3K signaling.BAG956 is effective against mutant FLT3-expressing cell lines and AML patient bone marrow cells.BAG956 and rapamycin/RAD001 were shown to combine in a nonantagonistic fashion against BCR-ABL- and mutant FLT3-expressing cells both in vitro and in vivo.NVP-BAG956 blocks cell proliferation, causing arrest in G1 phase of the cell cycle. Slows tumor progression in mouse xenograft models.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Harnessing the PI3K/Akt/mTOR pathway in T-cell acute lymphoblastic leukemia: eliminating activity by targeting at different levels.
Bressanin D. Oncotarget. 2012 Aug;3(8):811-23. PMID: 22885370.
Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors.
Marone R, et al. Mol Cancer Res. 2009 Apr;7(4):601-13. PMID: 19372588.
Potentiation of antileukemic therapies by the dual PI3K/PDK-1 inhibitor, BAG956: effects on BCR-ABL- and mutant FLT3-expressing cells.
Weisberg E, et al. Blood. 2008 Apr 1;111(7):3723-34. PMID: 18184863.
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