Free shipping on all orders over $ 500

NVP-BAG956

Cat. No. M4832
NVP-BAG956 Structure
Synonym:

BAG956

Size Price Availability Quantity
10mg USD 200 In stock
50mg USD 800 In stock
Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 427.50
Formula C28H21N5
CAS Number 853910-02-8
Purity >99%
Solubility DMSO
Storage at -20°C
References

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.

Related PDK1 Products
HS-173

HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM.

BX-912

BX912 is a selective potent PDK1 inhibitor with IC50 of 12 nM.

BX-795

BX795 is a potent and specific TBK1, IKKε and PDK-1 inhibitor with IC50 of 6 nM, 41 nM and 111 nM, respectively.

GSK2334470

GSK2334470 is a highly specific and potent inhibitor of PDK1 with IC50 of 10 nM.

OSU-03012

OSU-03012 is a novel and potent inhibitor of PDK-1 with an IC50 of 5 µM.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: NVP-BAG956, BAG956 supplier, PDK1, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.