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GNE-955
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GNE-955图片
CAS NO:1527523-39-2
包装与价格:
包装价格(元)
250mg电议
500mg电议

产品介绍
GNE-955是有效的泛Pim激酶抑制剂,Ki分别为18,110,8nM。
Cas No.1527523-39-2
Canonical SMILESCC1=CN=CC(C2=CC3=C(C=NN3C4=CC=C(OC)C(N5CCC[C@H](N)C5)=N4)C=N2)=N1
分子式C22H24N8O
分子量416.48
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.