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- Pim kinases
- GNE-955
GNE-955
GNE-955是有效的泛Pim激酶抑制剂，Ki分别为18，110，8nM。
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包装价格促销价数量
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250mg￥0.000.00- +
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500mg￥0.000.00- +
- 货号: ajcx12938
- CAS: 1527523-39-2
- 别名:
- 分子式: C22H24N8O
- 分子量: 416.48
- 纯度: ＞98%
- 溶解度: Soluble in DMSO
- 储存: Store at -20°C
- 库存: 现货
Background
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.
