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• 产品描述： Palbociclib (PD 0332991) isethionate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib isethionate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma

• 靶点： Cdk4/cyclin D3:9 nM (IC50);Cdk4/cyclin D1:11 nM (IC50);Cdk6/cyclin D2:16 nM (IC50);DYRK1A:2000 nM (IC50);MAPK:8000 nM (IC50);CDK

• 体内研究：
  Palbociclib isethionate (oral adminstration, 75 or 150 mg/kg, daily for 14 days) produces rapid tumor regressions and delays tumor growth. Palbociclib isethionate (oral adminstration, 90 mg/kg, daily for 12 days) reduces Treg numbers and the Treg:CD8 ratio in the spleen and lymph nodes in tumor-free mice, demonstrating the tumor-independent effects. Palbociclib isethionate (oral administration, 100 mg/kg, daily for 1 week) has potent antitumour effects in genetically engineered mosaic mouse model of liver cancer.

• 参考文献：
  1. Fry DW, et al. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther. 2004 Nov;3(11):1427-38. 2. Goel S, et al. CDK4/6 inhibition triggers anti-tumour immunity. Nature. 2017 Aug 24;548(7668):471-475. 3. Richard S Finn, et al. PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro. Breast Cancer Res. 2009;11(5):R77. 4. Bollard J, et al. Palbociclib (PD-0332991), a selective CDK4/6 inhibitor, restricts tumour growth in preclinical models of hepatocellular carcinoma. Gut. 2017 Jul;66(7):1286-1296.

• 溶解性： H2O  :  50  mg/mL  (87.16  mM;  Need  ultrasonic)    DMSO  :  10  mg/mL  (17.43  mM;  Need  ultrasonic)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.743 ml	8.716 ml	17.432 ml
  5 mM	0.349 ml	1.743 ml	3.486 ml
  10 mM	0.174 ml	0.872 ml	1.743 ml
  50 mM	0.035 ml	0.174 ml	0.349 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。

• 1. [IF=4.162] Suhua Wang et al."Design, Synthesis, and Biological Evaluation of 2-Anilino-4-Triazolpyrimidine Derivatives as CDK4/HDACs Inhibitors."Drug Des Dev Ther. 2022 Apr;16:1083-1097

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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 *