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• 产品描述： R547 is a potent, selective and orally active ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively

• 靶点： Cdk1/cyclin B:2 nM (Ki);CDK2/cyclinE:3 nM (Ki);CDK4/cyclin D:1 nM (Ki);cdk2/cyclin A:0.1 nM (IC50);CDK2/cyclinE:0.4 nM (IC50);Cdk1/cyclin B:0.2 nM (IC50);CDK3/Cyclin E:0.8 nM (IC50);CDK5/p35:0.1 nM (IC50);cdk6/cyclin D3:4 nM (IC50);CDK7/cyclin H:171 nM (IC50);GSK-3α:46 nM (IC50);GSK-3β:260 nM (IC50);Apoptosis;GSK-3;PKA;CDK

• 体内研究：
  R547 has significant in vivo efficacy with daily oral and once weekly i.v. dosing. R547 inhibits phosphorylation of retinoblastoma protein in tumors

• 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

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.265 ml	11.326 ml	22.653 ml
  5 mM	0.453 ml	2.265 ml	4.531 ml
  10 mM	0.227 ml	1.133 ml	2.265 ml
  50 mM	0.045 ml	0.227 ml	0.453 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *