S89235
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- 公司名稱 上海源葉生物科技有限公司
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- 更新時間 2024/7/3 18:39:49
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- 產(chǎn)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.
- 靶點： TNF-α
- 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(nèi)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.
- 細胞實驗： For assessment of cell apoptosis, Lymphoma cell lines are exposed to Pomalidomide (5 μg/mL) for 24 hours or 48 hours. The cells are stained with FITC-labeled Annexin V and propidium iodine. Cell apoptosis is analyzed by multicolor flow cytometric analysis using a fluorescence-activated cell sorter/FACStar Plus flow cytometer. Cells are scored as apoptotic if they are Annexin V–positive and propidium iodine–negative/positive (early and late apoptosis, respectively). For determination of cell proliferation, the Lymphoma cell lines are exposed to Pomalidomide (2.5, 5, 10, 20, and 40 μg/mL) for 24 hours or 48 hours. 1 μCi per well (96-well plate) of [3H]-thymidine is added and cells are incubated for another 18 hours. Cells are then harvested using the Harvest system into the 96-well glass filters and [3H]-thymidine uptake is measured using an automated scintillation counter.(Only for Reference) Cell lines: Raji, SU-DHL-4 and SU-DHL-10 cell lines
- 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
母液保存：分裝凍存,，避免反復凍融,；-20℃，1個月,；-80℃,，6個月（稀釋后溶液溫度低保存可能會析出,，盡量現(xiàn)用現(xiàn)配）
細胞實驗:先用DMSO溶解：再用培養(yǎng)基進行稀釋，稀釋過程建議分段進行,，避免濃度變化過快導致化合物析出。若稀釋過程中出現(xiàn)化合物析出的情況,， 可采用超聲的方法使其復溶,。在稀釋時要確保工作液中 DMSO 的終濃度盡量在0.1%以下，不要超過0.5%,，并設置相應濃度的DMSO對照組,。
動物實驗：先用DMSO溶解：再用水或者生理鹽水等去稀釋，稀釋過程建議分段進行,，避免濃度變化過快導致化合物析出,。若稀釋過程中出現(xiàn)化合物析出的情況， 可采用超聲的方法使其復溶,?？梢酝ㄟ^添加助溶劑來幫助溶解，比如植物油,、Tween80,、甘油、羧甲基纖維素鈉和PEG400等,。具體方式請參考文獻,。懸濁液可用于口服和腹腔注射，不會影響產(chǎn)品活性,。
- 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(chǎn)品我司僅能提供部分信息,，我司不保證所提供信息的性，僅供客戶參考交流研究之用,。
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