GNE-955 |
| رقم الكتالوجGC33253 |
GNE-955 هو مثبط قوي وفعال عن طريق الفم Pim kinase مع Kis 0.018 ، 0.11 ، 0.08 نانومتر لـ Pim1 ، Pim2 ، Pim3 ، على التوالي
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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