NU6027

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

NU6027  纯度: 99.35%

NU6027 是一种有效且的、ATP竞争性的 CDK1CDK2 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

NU6027 Chemical Structure

CAS No. : 220036-08-8

规格 价格 是否有货 数量
5 mg ¥700 In-stock
10 mg ¥1200 In-stock
25 mg ¥2500 In-stock
50 mg ¥4000 In-stock
100 mg ¥6000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

NU6027 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • PI3K/Akt/mTOR Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Glucose Metabolism Compound Library

生物活性

NU6027 is a potent and ATP-competitive inhibitor of both CDK1 and CDK2, with Kis of 2.5 µM and 1.3 µM, respectively. NU6027 is also a potent inhibitor of ATR and enhances hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner[1][2].

IC50 & Target[1][2]

CDK1

2.5 μM (Ki)

CDK2

1.3 μM (Ki)

ATR

 

体外研究
(In Vitro)

NU6027 (1 nM-100 µM; 48 h) inhibits the growth of human tumor cells with a GI50 of 10±6 µM[1].
NU6027 (0.1-25 µM; 24 h) inhibits ATR activity with an IC50 of 2.8 µM in GM847KD cells. NU6027 (1-10 µM; 24 h) inhibits ATR activity with an IC50 of 6.7±2.3 µM in MCF7 cells[2].
NU6027 (4 or 10 µM; 24 h) attenuates G2/M arrest following DNA damage in MCF7 cells[2].
NU6027 (10 µM; 24 h) significantly reduces RAD51 foci in both control and PF-01367338-treated V-C8 B2 cells[2].
NU6027 (4 µM; 24 h) causes 82% suppression of the increase in RAD51 foci-positive cells treated by PF-01367338[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[2]

Cell Line: MCF7 cells
Concentration: 0, 1, 5, 10 μM
Incubation Time: 24 h
Result: Inhibited CDK2-mediated pRbT821 by 42±27% compared with 70±12% inhibition of pCHK1S345 with the concentration of 10 µM.

分子量

251.28

Formula

C11H17N5O2

CAS 号

220036-08-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 12.5 mg/mL (49.75 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.9796 mL 19.8981 mL 39.7962 mL
5 mM 0.7959 mL 3.9796 mL 7.9592 mL
10 mM 0.3980 mL 1.9898 mL 3.9796 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.25 mg/mL (4.97 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (4.97 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.25 mg/mL (4.97 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (4.97 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务