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NU6027

NU6027用途

NU6027 是一种有效且的、ATP竞争性的 CDK1 和 CDK2 的抑制剂,Ki 值分别为 2.5 µM 和 1.3 µM。NU6027 也是 ATR 的有效抑制剂,以 ATR 依赖性方式增强羟基脲和顺铂的细胞毒性。

NU6027名称

[ CAS 号 ]:
220036-08-8

[ 英文名 ]:
NU6027

[英文别名 ]:

NU6027
NW1
1e1x

NU6027生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 细胞周期/DNA损伤 >> ATM/ATR

信号通路 >> 细胞周期/DNA损伤 >> CDK

信号通路 >> PI3K/Akt/mTOR 信号通路 >> ATM/ATR

[ 靶点 ]

CDK1:2.5 μM (Ki)

CDK2:1.3 μM (Ki)

ATR

[体外研究]

NU6027(1 nM-100µM；48 h)抑制GI50为10±6µM的人类肿瘤细胞的生长[1]。NU6027(0.1-25µM；24 h)抑制GM847KD细胞中ATR活性,IC50为2.8µM。NU6027(1-10µM；24小时)抑制MCF7细胞中ATR活性,IC50为6.7±2.3µM[2]。NU6027(4或10µM；24 h)减弱MCF7细胞DNA损伤后的G2/M阻滞[2]。NU6027(10µM；24小时)显著降低对照组和PF-01367338处理的V-C8 B2细胞中的RAD51病灶[2]。NU6027(4µM；24小时)可抑制PF-01367338治疗的RAD51病灶阳性细胞的增加82%。Western Blot分析[2]细胞系：MCF7细胞浓度：0、1、5、10μM孵育时间：24 h结果：对CDK2介导的pRbT821的抑制率为42±27%,而pCHK1S345的抑制率为70±12%。

[参考文献]

[1]. Arris CE, et, al. Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles. J Med Chem. 2000 Jul 27; 43(15): 2797-804.

[2]. Peasland A, et, al. Identification and evaluation of a potent novel ATR inhibitor, NU6027, in breast and ovarian cancer cell lines. Br J Cancer. 2011 Jul 26;105(3):372-81.

NU6027物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
549.2±60.0 °C at 760 mmHg

[ 熔点 ]:
252.5-253.7 °C(lit.)

[ 分子式 ]:
C₁₁H₁₇N₅O₂

[ 分子量 ]:
251.285

[ 闪点 ]:
286.0±32.9 °C

[ 精确质量 ]:
251.138229

[ PSA ]:
117.21000

[ LogP ]:
3.71

[ 外观性状 ]:
lavender

[ 蒸汽压 ]:
0.0±1.5 mmHg at 25°C

[ 折射率 ]:
1.699

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
DMSO: 15 mg/mL

NU6027MSDS

详细MSDS(安全技术说明书)

NU6027安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

NU6027文献

Ataxia telangiectasia mutated and Rad3 related (ATR) protein kinase inhibition is synthetically lethal in XRCC1 deficient ovarian cancer cells.

PLoS ONE 8 , e57098, (2013)

Ataxia telangiectasia mutated and Rad3 Related (ATR) protein kinase is a key sensor of single-stranded DNA associated with stalled replication forks and repair intermediates generated during DNA repai...

Identification and evaluation of a potent novel ATR inhibitor, NU6027, in breast and ovarian cancer cell lines.

Br. J. Cancer 105 , 372-81, (2011)

The ataxia telangiectasia mutated and Rad3-related kinase (ATR) has a key role in the signalling of stalled replication forks and DNA damage to cell cycle checkpoints and DNA repair. It has long been ...

Kinetically-defined component actions in gene repression.

PLoS Comput. Biol. 11(3) , e1004122, (2015)

Gene repression by transcription factors, and glucocorticoid receptors (GR) in particular, is a critical, but poorly understood, physiological response. Among the many unresolved questions is the diff...

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