BX517

Names

[ Name ]:
BX517

[Synonym ]:
5-Ureido-3-[1-(pyrrol-2-yl)ethylidene]indolin-2-one
Urea, [2,3-dihydro-2-oxo-3-[1-(1H-pyrrol-2-yl)ethylidene]-1H-indol-5-yl]-
PDK-1 INHIBITOR II
BX517

Biological Activity

[Description]:

BX517 is a potent and selective inhibitor of PDK1 with IC50 of 6 nM.

[Related Catalog]:

Signaling Pathways >> PI3K/Akt/mTOR >> PDK-1

Research Areas >> Cancer

[Target]

IC50: 6 nM (PDK1)

[In Vitro]

BX-517 blocks activation of Akt in tumor cells, is potent with IC50 of 0.1-1.0 μM[1]. BX-517 blocks AKT2 activation in cells with submicromolar potency. BX-517 is 100-fold selective or better against a panel of seven additional Ser/Thr and Tyr kinases[2].

[References]

[1]. Islam I, et al. Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3819-25.

[2]. Islam I, et al. Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3814-8.

[Related Small Molecules]

BX-795 | GSK2334470 | PS48 | MP7 | BX-912 | OSU-03012 (AR-12)

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₅H₁₄N₄O₂

[ Molecular Weight ]:
282.29700

[ Exact Mass ]:
282.11200

[ PSA ]:
100.01000

[ LogP ]:
3.29940

[ Storage condition ]:
2-8℃