产品说明书
Ciforadenant
 |
同义名 : | CPI-444;V81444 |
| CAS号 : | 1202402-40-1 | |
| 货号 : | A186100 | |
| 分子式 : | C20H21N7O3 | |
| 纯度 : | 99%+ | |
| 分子量 : | 407.426 | |
| MDL号 : | MFCD31540410 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 65 mg/mL(159.54 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
|
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Adenosine signaling through the A2A adenosine receptor(A2AR) on immune cells is a critical regulator of inflammation and immune response which has been shown to suppress antitumor immunity and limit the efficacy of immunotherapy, chemotherapy, adoptive cell transfer therapies, and vaccines in preclinical models. CPI-444 is an orally administered antagonist of the A2AR with a Ki of 3.54 nM. C57BL/6 mice immunized with vaccinia-OVA showed a signifcant enhancement in the antigen-specifc CD8+ T cell response when treated with CPI-444 (10 mg/kg, p.o. daily for 5 days starting 1 day post-infection) compared with models[2]. Anti-PD-1 and CPI-444(100 mg/kg, 12 days) combination treatment showed a significant improvement in tumor regression and animal survival in both CT26 and MC38 tumor models, compared with anti-PD-1 treatment alone. Phase 1b clinical trial in patients with non-small cell lung, melanoma, renal, triple negative breast, and other (head and neck, colorectal [MSI-H], bladder) tumors demonstrated that NECA(adenosine analog) signaling was robustly inhibited at the doses selected in CPI-444 treatment[3]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT03708224 | Cancer Carcin... 展开 >>oma Squamous Cell Carcinoma Head and Neck Cancer 收起 << | Phase 2 | Not yet recruiting | November 30, 2025 | United States, California ... 展开 >> University of San Francisco, California San Francisco, California, United States, 94115 收起 << |
| NCT03337698 | Carcinoma, Non-Small-Cell Lung | Phase 1 Phase 2 | Recruiting | April 20, 2022 | United States, Connecticut ... 展开 >> Smilow Cancer Hospital at Yale New Haven Recruiting New Haven, Connecticut, United States, 06510 United States, Massachusetts Massachusetts General Hospital Not yet recruiting Boston, Massachusetts, United States, 02114 Dana-Farber Cancer Institute Recruiting Boston, Massachusetts, United States, 02215 United States, New York Columbia University Medical Center; Research Pharmacy, Irving Pavillion, Ip 7-749 Recruiting New York, New York, United States, 10032 United States, Tennessee Sarah Cannon Research Institute Recruiting Nashville, Tennessee, United States, 37203 Australia, Victoria Peter Mac Callum Cancer Center Recruiting East Melbourne, Victoria, Australia, 3002 France Centre Léon Bérard Recruiting Lyon, France, 69008 Hôpital Nord Not yet recruiting Marseille, France, 13915 Institut Universitaire du Cancer de Toulouse-Oncopole; PHARMACIE Recruiting Toulouse, France, 31100 Korea, Republic of Seoul National University Hospital Recruiting Seoul, Korea, Republic of, 03080 Severance Hospital, Yonsei University Health System; Pharmacy Recruiting Seoul, Korea, Republic of, 03722 University of Ulsan College of Medicine - Asan Medical Center (AMC) - Asan Cancer Center (ACC) Recruiting Songpa-gu, Korea, Republic of, 05505 Spain Clínica Universidad de Navarra Recruiting Pamplona, Navarra, Spain, 31620 Hospital Universitari Vall d'Hebron Recruiting Barcelona, Spain, 08035 Fundación Jimenez Díaz Recruiting Madrid, Spain, 28040 South Texas Accelerated Research Therapeutics Madrid - CIOCC - Universitario Sanchinarro Recruiting Madrid, Spain, 28050 United Kingdom Barts Cancer Institute Recruiting London, United Kingdom, E1 2AT Royal Marsden Hospital; Institute of Cancer Research Recruiting Sutton, United Kingdom, SM2 5PT 收起 << |
| NCT03454451 | Non-Small Cell Lung Cancer ... 展开 >> Renal Cell Cancer Colorectal Cancer Triple Negative Breast Cancer Cervical Cancer Ovarian Cancer Pancreatic Cancer Endometrial Cancer Sarcoma Squamous Cell Carcinoma of the Head and Neck Bladder Cancer Metastatic Castration Resistant Prostate Cancer 收起 << | Phase 1 | Recruiting | December 2023 | United States, Connecticut ... 展开 >> Yale School of Medicine Recruiting New Haven, Connecticut, United States, 06519 Contact: Site Coordinator 203-785-3482 ycci@yale.edu Principal Investigator: Patricia LoRusso, MD United States, Florida University of Miami Recruiting Miami, Florida, United States, 33136 Contact: Study Coordinator 305-243-0865 txl351@med.miami.edu Principal Investigator: Jaime Merchan, MD United States, Illinois The University of Chicago Recruiting Chicago, Illinois, United States, 60637 Contact: Site Coordinator 773-702-1835 mweist@medicine.bsd.uchicago.edu Principal Investigator: Jason Luke, MD United States, New York Icahn School of Medicine at Mount Sinai Recruiting New York, New York, United States, 10029 Contact: Site Coordinator 212-824-7309 ccto@mssm.edu Principal Investigator: Thomas Marron, MD United States, North Carolina Carolina BioOncology Institute Recruiting Huntsville, North Carolina, United States, 28078 Contact: Study Coordinator 704-947-6599 info@carolinabiooncology.org Principal Investigator: John Powderly United States, Oklahoma University of Oklahoma - Stephenson Cancer Center Recruiting Oklahoma City, Oklahoma, United States, 73104 Contact: Site Coordinator 405-271-1112 SCC-Clinical-Trials-Office@ouhsc.edu Principal Investigator: Abhishek Tripathi, MD United States, Tennessee Sarah Cannon Research Institute Recruiting Nashville, Tennessee, United States, 37203 Contact: Site Coordinator 615-329-7274 asksarah@sarahcannon.com Principal Investigator: Melissa Johnson, MD United States, Texas Mary Crowley Cancer Research Recruiting Dallas, Texas, United States, 75230 Contact: Study Coordinator 972-566-3000 information@marycrowley.org Principal Investigator: Minal Barve, MD United States, Wisconsin Froedtert Hospital & Medical College of Wisconsin Recruiting Milwaukee, Wisconsin, United States, 53226 Contact: Site Coordinator 414-805-8900 CCCTO@mcw.edu Principal Investigator: Matthew Riese, MD 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.45mL 0.49mL 0.25mL |
12.27mL 2.45mL 1.23mL |
24.54mL 4.91mL 2.45mL |
| 参考文献 |
|---|