R547

• 常用名: R547
• 英文名: R547
• CAS号: 741713-40-6
• 分子量: 441.45200
• 密度: 1.49
• 沸点: 703.7ºC at 760 mmHg
• 分子式: C₁₈H₂₁F₂N₅O₄S
• 熔点: N/A
• 闪点: 379.4ºC

R547用途

R547是ATP竞争性CDK1,2,4抑制剂,Ki分别为2 nM,3 nM和1 nM。

R547名称

• 中文名: [4-氨基-2-[(1-甲磺酰基哌啶-4-基)氨基]嘧啶-5-基](2,3-二氟-6-甲氧基苯基)甲酮
• 英文名: [4-amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl]-(2,3-difluoro-6-methoxyphenyl)methanone
• 中文别名: 大麦芽碱.对二甲氨乙基苯酚

R547生物活性

• 描述: R547是ATP竞争性CDK1,2,4抑制剂,Ki分别为2 nM,3 nM和1 nM。
• 相关类别:
  研究领域 >> 癌症
• 靶点:

  Cdk1/cyclin B:2 nM (Ki)

  CDK4/cyclin D:1 nM (Ki)

  CDK2/cyclinE:3 nM (Ki)

• 参考文献:

  [1]. Chu XJ, DePinto W, Bartkovitz D, So SS, Vu BT, Packman K, Lukacs C, Ding Q, Jiang N, Wang K, Goelzer P, Yin X, Smith MA, Higgins BX, Chen Y, Xiang Q, Moliterni J, Kaplan G, Graves B, Lovey A, Fotouhi N.Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4

  [2]. Bayés M, Rabasseda X, Prous JR.Gateways to clinical trials.Methods Find Exp Clin Pharmacol. 2007 Jul-Aug;29(6):427-37.

  [3]. Martin F, Thomson TM, Sewer A, Drubin DA, Mathis C, Weisensee D, Pratt D, Hoeng J, Peitsch MC.Assessment of network perturbation amplitudes by applying high-throughput data to causal biological networks.BMC Syst Biol. 2012 May 31;6:54.

  [4]. DePinto, Wanda et al In vitro and in vivo activity of R547: a potent and selective cyclin-dependent kinase inhibitor currently in phase I clinical trials Molecular Cancer Therapeutics (2006), 5(11), 2644-2658

  [5]. Jones, Clifford D.; Andrews, David M. Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors Bioorganic & Medicinal Chemistry Letters (2008), 18(24), 6486-6489

R547物理化学性质

• 密度: 1.49
• 沸点: 703.7ºC at 760 mmHg
• 分子式: C₁₈H₂₁F₂N₅O₄S
• 分子量: 441.45200
• 闪点: 379.4ºC
• 精确质量: 441.12800
• PSA: 135.89000
• LogP: 3.08540
• 外观性状: 粉末
• 折射率: 1.62
• 储存条件: -20℃

R547安全信息

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

R547英文别名

• (4-Amino-2-{[1-(methylsulfonyl)-4-piperidinyl]amino}-5-pyrimidinyl)(2,3-difluoro-6-methoxyphenyl)methanone
• Methanone, [4-amino-2-[[1-(methylsulfonyl)-4-piperidinyl]amino]-5-pyrimidinyl](2,3-difluoro-6-methoxyphenyl)-
• R547
• RO-4584820
• cc-270
• pound not R 547
• R 547
• (4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino)pyrimidin-5-yl)(2,3-difluoro-6-methoxyphenyl)methanone
• [4-amino-2-(1-methanesulfonyl-piperidin-4-ylamino)-pyrimidin-5-yl]-(2,3-difluoro-6-methoxy-phenyl)-methanone
• Ro 4584820
• (4-Amino-2-{[1-(methylsulfonyl)piperidin-4-yl]amino}pyrimidin-5-yl)(2,3-difluoro-6-methoxyphenyl)methanone