• 產品描述：

  Pomalidomide, also known as CC4047, is an orally bioavailable derivative of thalidomide with potential immunomodulating, antiangiogenic and antineoplastic activities. Although its exact mechanism of action has yet to be fully elucidated, pomalidomide appears to inhibit TNF-alpha production, enhance the activity of T cells and natural killer (NK) cells and enhance antibody-dependent cellular cytotoxicity (ADCC). Pomalidomide was approved on February 8, 2013 as a treatment for relapsed and refractory multiple myeloma.

• 體外研究： Pomalidomide also inhibits Whole Blood TNF-α with IC50 of 25 nM. Exposure of lymphoma cells to Pomalidomide (CC-4047) leads to 40% decrease in cell proliferation when compared with vehicle-treated controls. Pomalidomide inhibits by 40% the DNA synthesis of Raji cells (P=0.036). In both CD4+ and CD8+ cells, Pomalidomide (CC-4047) is the most potent IL-2-elevator, followed by CC-6032 and CC-5013. Pomalidomide is significantly more potent than CC-5013 at elevating IL-2, IL-5, and IL-10, and slightly more potent than CC-5013 at elevating IFN-γ.

• 體內研究： The administration of Pomalidomide (CC-4047) for two consecutive days before mAb therapy enhances the antitumor activity of Rituximab and doubled the median survival of lymphoma-bearing mice. Statistically, significant differences are observed between animals treated with Rituximab versus Pomalidomide+Rituximab. The median survival time of animals treated with Pomalidomide and Rituximab is longer (median survival, 74 days; 95% CI, 70-78) than those treated with Rituximab monotherapy (median survival, 38 days; 95% CI, 26-50; log-rank test, P=0.002). The administration of CC-5013 or Pomalidomide for two consecutive days leads to a significant increase in the number of circulating NK cells as shown by flow cytometry analysis, in lymphoma-bearing SCID mice. Following a 50 mg/kg PO administration of Pomalidomide (POM) to rats, unbound concentrations in blood reach a Cmax value of 1100±82 ng/mL at 4.6±2.4 hours, with a concomitant AUC(0-10) value of 6800±2000 ng?hr/mL. Unbound POM in the brain, however, has a Cmax value of 430±63 ng/mL at 4.1±1.5 hours and an AUC(0-10) value of 2700±740 ng?hr/mL, giving an unbound AUCbrain to AUCblood ratio of 0.39±0.03. These values are consistent with excellent blood-brain-barrier penetration. The results obtained in this study are consistent with those seen in a concurrent study looking at whole brain POM content following its oral administration to mice.

• 參考文獻：
  1: Elkinson S, McCormack PL. Pomalidomide: First Global Approval. Drugs. 2013 Apr 10. [Epub ahead of print] PubMed PMID: 23572409.
  
  2: Traynor K. Pomalidomide approved for multiple myeloma. Am J Health Syst Pharm. 2013 Mar 15;70(6):474. doi: 10.2146/news130020. PubMed PMID: 23456394.
  
  3: Henry JY, Labarthe MC, Meyer B, Dasgupta P, Dalgleish AG, Galustian C. Enhanced cross-priming of naive CD8+ T cells by DCs treated by the IMiDs(??) immunomodulatory compounds Lenalidomide and Pomalidomide. Immunology. 2013 Feb 1. doi: 10.1111/imm.12087. [Epub ahead of print] PubMed PMID: 23374145.
  
  4: Ellis PM, Jungnelius U, Zhang J, Fandi A, Beck R, Shepherd FA. A Phase I Study of Pomalidomide (CC-4047) in Combination with Cisplatin and Etoposide in Patients with Extensive-Stage Small-Cell Lung Cancer. J Thorac Oncol. 2013 Apr;8(4):423-8. doi: 10.1097/JTO.0b013e318282707b. PubMed PMID: 23370364.

• 溶解度： DMSO：54  mg/mL  (197.62  mM)；Water  ：Insoluble；Ethanol    ：Insoluble

• 保存條件： 2-8℃

• 配置溶液濃度參考：
  

  	1mg	5mg	10mg
  1 mM	3.66 ml	18.299 ml	36.598 ml
  5 mM	0.732 ml	3.66 ml	7.32 ml
  10 mM	0.366 ml	1.83 ml	3.66 ml
  50 mM	0.073 ml	0.366 ml	0.732 ml

• 注意：部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

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本計算器可幫助您計算出特定溶液中溶質的質量、溶液濃度和體積之間的關系，公式為：

質量 (mg) = 濃度 (mM) x 體積 (mL) x 分子量 (g/mol)

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