444723-13-1|4-((6-(Cyclohexylmethoxy)-7H-purin-2-yl)amino)-N,N-diethylbenzamide|CsnPharm

CAS No.: 444723-13-1

NU6140 Catalog No. CSN25344

Synonyms: NU6140

NU6140 is a selective CDK2 inhibitor with IC50 value of 0.94μM, as well as potently inhibits Aurora kinase A/B with IC50 values of 0.035 and 0.067μM, respectively.

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技术信息

生物活性

描述CDK2 (Cyclin Dependent Kinase 2) is a protein coding gene. Disease associated with CDK2 including breast cancer and retinoblastoma. This gene encodes a member of a family of serine/threonine protein kinases thata participate in cell cycle regulation. Activity if this protein is especially critical during the G1 to S phase transition. NU 6140 is a cyclin-dependent kinase 2 (Cdk2) inhibitor (IC50 = 0.41 μM) that demonstrates 10- to 36-fold selectivity against Cdk2-cyclin A compared to Cdk1-cyclin B, Cdk4-cyclin D, Cdk5-p25, or Cdk7-cyclin H^[1]. NU6140 also potently inhibits Aurora A and Aurora B, with IC50s of 67 and 35 nM, respectively. NU6140 enhances the apoptotic effect, with anti-cancer activity^[2]. Both hES and hEC cells responded to NU6140 treatment by induced apoptosis and a decreased expression of NANOG, OCT4, and SOX2 in surviving cells. NU6140 treatment arrested hES and hEC cells in the G2 phase and inhibited entry into the M phase as evidenced by no significant increase in histone 3 phosphorylation^[3].
参考文献

[1] Pennati, M., Campbell, A.J., Curto, M., et al. Potentiation of paclitaxel-induced apoptosis by the novel cyclin-dependent kinase inhibitor NU6140: A possible role for survivin down-regulation. Mol. Cancer Ther. 2005. 4(9), 1328-1337.
[2] Jorda R, et al. How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? Med Chem. 2018. 61(20), 9105-9120.
[3] Ade Kallas,et al. Assessment of the Potential of CDK2 Inhibitor NU6140 to Influence the Expression of Pluripotency Markers NANOG, OCT4, and SOX2 in 2102Ep and H9 Cells. Int J Cell Biol. 2014.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3667 mL
- 11.8337 mL
- 23.6673 mL
- 5 mM
- 0.4733 mL
- 2.3667 mL
- 4.7335 mL
- 10 mM
- 0.2367 mL
- 1.1834 mL
- 2.3667 mL

技术信息

CAS号	444723-13-1	储存条件	粉末 Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C23H30N6O2	运输	蓝冰
分子量	422.52	别名	NU6140

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