I-BET151 |CAS:1300031-49-5 Probechem Biochemicals

Chemical Structure : I-BET151

CAS No.: 1300031-49-5

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I-BET151 (GSK1210151A;I-BET 151;GSK-1210151A;GSK 1210151A)

货号: PC-43414Not For Human Use, Lab Use Only.

I-BET151 (GSK1210151A) is a potent, selective BET bromodomain inhibitor with IC50 of 0.5, 0.25 and 0.79 uM for BRD2, BRD3 and BRD4 in FP assays, shows no effect on the 23 other bromodomain proteins including MLL.

规格	价格	库存
5 mg	￥980	In stock
10 mg	￥1380	In stock
25 mg	￥2380	In stock
50 mg	￥3980	In stock
100 mg		Get quote

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生物&药学活性

I-BET151 (GSK1210151A) is a potent, selective BET bromodomain inhibitor with IC50 of 0.5, 0.25 and 0.79 uM for BRD2, BRD3 and BRD4 in FP assays, shows no effect on the 23 other bromodomain proteins including MLL.
I-BET151 (GSK1210151A) demonstrates potent efficacy against cell lines harbouring different MLL-fusions (MOLM13 cell IC50=120 nM, MV4:11 cell IC50=26 nM).
I-BET151 (GSK1210151A) induces early cell cycle arrest and apoptosis, selectively abrogates BRD3/4 recruitment to chromatin。
I-BET151 (GSK1210151A) shows significant therapeutic value and survival benefit in mouse models of murine MLL-AF9 and human MLL-AF4 leukaemia.

物理化学性质&存储条件

分子量	415.4445
分子式	C23H21N5O3
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
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2H-Imidazo[4,5-c]quinolin-2-one, 7-(3,5-dimethyl-4-isoxazolyl)-1,3-dihydro-8-methoxy-1-[(1R)-1-(2-pyridinyl)ethyl]-

参考文献

1. Dawson MA, et al. Nature. 2011 Oct 2;478(7370):529-33.

2. Mirguet O, et al. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2963-7.

3. Chaidos A, et al. Blood. 2014 Jan 30;123(5):697-705.

4. Wyspiańska BS, et al. Leukemia. 2014 Jan;28(1):88-97.

I-BET151 (GSK1210151A;I-BET 151;GSK-1210151A;GSK 1210151A)

生物&药学活性

物理化学性质&存储条件

参考文献

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I-BET151 (GSK1210151A;I-BET 151;GSK-1210151A;GSK 1210151A)

生物&药学活性

物理化学性质&存储条件

参考文献

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