产品名称

英文名称：I-BET151

同义词

1300031-49-5、I-BET151、GSK1210151A、I-BET151 (GSK1210151A)、7-(3,5-Dimethylisoxazol-4-yl)-8-methoxy-1-((R)-1-(pyridin-2-yl)ethyl)-1H-imidazo[4,5-c]quinolin-2(3H)-one、GSK1210151A (I-BET151)、CHEMBL2017291、(R)-7-(3,5-dimethylisoxazol-4-yl)-8-methoxy-1-(1-(pyrid、7-(3,5-二甲基-4-异噁唑基)-1,3-二氢-8-甲氧基-1-[(1R)-1-(2-吡啶基)乙基]-2H-咪唑并[4,5-C]喹啉-2-酮

产品性质

CAS编号：1300031-49-5

分子式：C23H21N5O3

分子量：415.44

PubChem编号：52912189

别名：7-(3,5-二甲基-4-异噁唑基)-1,3-二氢-8-甲氧基-1-[(1R)-1-(2-吡啶基)乙基]-2H-咪唑并[4,5-C]喹啉-2-酮

英文别名：1300031-49-5|I-BET151|GSK1210151A|I-BET151 (GSK1210151A)|7-(3,5-Dimethylisoxazol-4-yl)-8-methoxy-1-((R)-1-(pyridin-2-yl)ethyl)-1H-imidazo[4,5-c]quinolin-2(3H)-one|GSK1210151A (I-BET151)|CHEMBL2017291|(R)-7-(3,5-dimethylisoxazol-4-yl)-8-methoxy-1-(1-(pyrid

规格或纯度：≥98%

英文名称：I-BET151

生化机理：I-BET151 is a BET bromodomain inhibitor; I-BET151 blocks recruitment of BET to chromatin. I-BET151 induces apoptosis and G0/G1 cell cycle arrest in MLL-fusion leukemic cell lines in vitro (IC50 values are 15, 26, 120 and 192 nM for NOMO1, MV4;11, MOLM13 and RS4;11 cell lines respectively). I-BET151 reduces BCL2 expression in NOMO1 cells. I-BET151 improves survival in two rodents models of MLL-fusion leukemia in vivo.I-BET151 is an isoxazole class pan-BET family inhibitor, blocking BRD2, BRD3 and BRD4 with IC 50 values of 0.5, 0.25 and 0.79 µM, respectively. Specifically, I-BET151 induces apoptosis via reduced expression of BCL2 or triggers G 0 /G 1 cell cycle arrest

储存温度：2-8°C储存

运输条件：冰袋运输

备注：有毒，请参阅SDS以获取更多信息。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。

产品介绍：产品介绍I-BET151 (GSK1210151A) 是一种 BET 溴结构域 (BET bromodomain) 抑制剂，抑制 BRD4，BRD2 和 BRD3 的 pIC50 分别为 6.1，6.3 和 6.6。产品应用GSK1210151A 或 I-BET151 已用于研究其在治疗 MLL（混合谱系白血病）-融合性白血病中对 BET（溴结构域和额外末端）募集染色质的抑制作用。

IUPAC Name：7-(3,5-dimethyl-1,2-oxazol-4-yl)-8-methoxy-1-[(1R)-1-pyridin-2-ylethyl]-3H-imidazo[4,5-c]quinolin-2-one

INCHI：InChI=1S/C23H21N5O3/c1-12-21(14(3)31-27-12)16-9-18-15(10-20(16)30-4)22-19(11-25-18)26-23(29)28(22)13(2)17-7-5-6-8-24-17/h5-11,13H,1-4H3,(H,26,29)/t13-/m1/s1

InChi Key：VUVUVNZRUGEAHB-CYBMUJFWSA-N

Canonical SMILES：CC1=C(C(=NO1)C)C2=C(C=C3C(=C2)N=CC4=C3N(C(=O)N4)C(C)C5=CC=CC=N5)OC

Isomeric SMILES：CC1=C(C(=NO1)C)C2=C(C=C3C(=C2)N=CC4=C3N(C(=O)N4)[C@H](C)C5=CC=CC=N5)OC

WGK Germany：3

PubChem CID：52912189

ChEMBL Ligand：CHEMBL2017291

CAS Registry No.：1300031-49-5

RCSB PDB Ligand：1GH

溶解性：DMSO 100 mM Ethanol 100 mM

象形图：

信号词：Danger

危险声明：H301 Toxic if swallowed

预防措施声明：P321,P405,P501,P264,P270,P330,P301+P316

产品包装