850717-64-5

850717-64-5 structure

Name: BX517
Chemical Name: Urea, N-[2,3-dihydro-2-oxo-3-[1-(1H-pyrrol-2-yl)ethylidene]-1H-indol-5-yl]
CAS Number: 850717-64-5
Molecular Formula: C₁₅H₁₄N₄O₂
Molecular Weight: 282.29700
Catalog: Signaling Pathways PI3K/Akt/mTOR PDK-1
Create Date: 2017-09-17 02:56:45
Modify Date: 2024-01-10 14:21:04
BX517 is a potent and selective inhibitor of PDK1 with IC50 of 6 nM.

Name	Urea, N-[2,3-dihydro-2-oxo-3-[1-(1H-pyrrol-2-yl)ethylidene]-1H-indol-5-yl]
Synonyms	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

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.