GNE-955

Names

[ CAS No. ]:
1527523-39-2

[ Name ]:
GNE-955

Biological Activity

[Description]:

GNE-955 is a potent pan Pim kinase inhibitor with Kis of 18, 110, 8 nM for Pim1, Pim2, Pim3, respectively.

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> Pim

[Target]

PIM1:18 nM (Ki)

PIM2:110 nM (Ki)

PIM3:8 nM (Ki)

[In Vitro]

MM.1S myeloma cell line treated with a dose range of GNE-955 reveals a constellation of PIM downstream signaling events consistent with inhibition of Pim kinases[1].

[In Vivo]

GNE-955 has excellent bioavailability in rat. Rat clearance of GNE-955 is moderate at 34 mL /min/kg with good oral exposure[1].

[References]

[1]. Wang X, et al. Discovery of 5-Azaindazole (GNE-955) as a Potent Pan-Pim Inhibitor with Optimized Bioavailability. J Med Chem. 2017 May 25;60(10):4458-4473.

Chemical & Physical Properties

No Any Chemical & Physical Properties

Related Compounds

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