CAS NO: | 1936422-33-1 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | GNE-781 is an orally active, highly potent and selectiveCBPinhibitor with anIC50of 0.94 nM in TR-FRET assay. GNE-781 also inhibitsBRETandBRD4(1)withIC50s of 6.2 nM and 5100 nM, respectively. GNE-781 displays antitumor activity in an MOLM-16 AML xenograft model[1]. | ||||||||||||||||
IC50& Target | IC50: 0.94 nM (CBP), 6.2 nM (BRET), 5100 nM (BRD4(1))[1] | ||||||||||||||||
体外研究 (In Vitro) | GNE-781 is a highly advanced potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element binding protein, binding protein (CBP). GNE-781 reduces FOXP3 (forkhead box P3) transcript levels. Examination of a subset of bromodomains reveals that GNE-781 is exquisitely selective for CBP/P300 and is remarkably selective for CBP (5425-fold) and P300 (4250-fold). GNE-781 demonstrates an appropriate balance of cell potency, selectivity (5425-fold over BRD4(1))[1]. | ||||||||||||||||
体内研究 (In Vivo) | GNE-781 (3-30 mg/kg; p.o.; twice daily for 21 days) has tumor growth inhibition (%TGI) is 73%, 71%, and 89% at 3, 10, and 30 mg/kg, respectively in SCID beige mice with MOLM-16 AML xenografts[1]. | ||||||||||||||||
分子量 | 525.59 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C27H33F2N7O2 | ||||||||||||||||
CAS 号 | 1936422-33-1 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | -20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : 100 mg/mL(190.26 mM;Need ultrasonic) 配制储备液
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