GNE-955 |
| Catalog No.GC33253 |
GNE-955는 Pim1, Pim2, Pim3에 대해 각각 Kis가 0.018, 0.11, 0.08 nM인 강력한 경구 활성 pan Pim 키나제 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1527523-39-2
Sample solution is provided at 25 µL, 10mM.
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GNE-955 is a potent pan Pim kinase inhibitor with Kis of 18, 110, 8 nM for Pim1, Pim2, Pim3, respectively.
Pim kinases have been identified as promising therapeutic targets for hematologic-oncology indications, including multiple myeloma and certain leukemia. 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].
GNE-955 has excellent bioavailability in rat. Rat clearance of GNE-955 is moderate at 34 mL /min/kg with good oral exposure[1].
[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.
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