GNE-781 |Cas:1936422-33-1 Buy GNE-781 from ProbeChem, Global Biochemicals Supplier

Chemical Structure : GNE-781

CAS No.: 1936422-33-1

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GNE-781 (GNE781;GNE 781)

货号: PC-60306Not For Human Use, Lab Use Only.

GNE-781 (GNE781) is a potent, selective, non-CNS penetrant, orally active CBP/p300 bromodomain inhibitor with IC50 of 0.94/1.2 nM in TR-FRET assays.

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5 mg	￥2880	In stock
10 mg	￥4580	In stock
25 mg		Get quote
100 mg		Get quote

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生物&药学活性

GNE-781 (GNE781) is a potent, selective, non-CNS penetrant, orally active CBP/p300 bromodomain inhibitor with IC50 of 0.94/1.2 nM in TR-FRET assays.
GNE-781 exhibits high selectivity over BRD4 (1) (>5 uM) and other BRDs.
GNE-781 suppresses Myc transcript levels in cellular assays with EC50 of 6.6 nM.
GNE-781 displays antitumor activity in an AML tumor model and decreases Foxp3 transcript levels in a dose dependent manner.

物理化学性质&存储条件

分子量	525.605
分子式	C27H33F2N7O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
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Solubility	10 mM in DMSO
Chemical Name/SMILES	3-[7-(Difluoromethyl)-6-(1-methylpyrazol-4-yl)-3,4-dihydro-2H-quinolin-1-yl]-N-methyl-1-tetrahydropyran-4-yl-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carboxamide

参考文献

1. Romero FA, et al. J Med Chem. 2017 Nov 22;60(22):9162-9183.

GNE-781 (GNE781;GNE 781)

生物&药学活性

物理化学性质&存储条件

参考文献

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GNE-781 (GNE781;GNE 781)

生物&药学活性

物理化学性质&存储条件

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