ARQ 531
产品说明书
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同义名 : | Nemtabrutinib;MK-1026 |
| CAS号 : | 2095393-15-8 | |
| 货号 : | A630399 | |
| 分子式 : | C25H23ClN4O4 | |
| 纯度 : | 99%+ | |
| 分子量 : | 478.928 | |
| MDL号 : | MFCD31692379 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL(104.4 mM)，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 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | The Bruton’s tyrosine kinase (BTK) has been shown to drive the development of chronic lymphocytic leukemia (CLL). ARQ 531 is an ATP-competitive, reversible inhibitor of BTK with IC50 values of 0.85 and 0.39nM for wild-type BTK and C481S BTK, respectively. ARQ 531 also shows inhibitory activities against Src family kinases (LCK, YES, BLK, HCK, LYNa, FGR, FYN, FRK), TEK kinases (BMX, TEC, TXK), and Trk kinases (TrkB, TrkA, TrkC) with IC50 values ranging from 2.5–48nM. ARQ 531 at 0.1, 1, and 10μM decreased the viability of CLL cells by 19%, 40%, and 59%, respectively. Treatment with 1μM ARQ 531 significantly decreased the transcription of MYC, MCL1, and CD40 in CLL cells by 73%, 23%, 40%, respectively, compared to the vehicle controls. ARQ 531 at 1μM also decreased the migration of primary CLL cells towards CXCL12 and CXCL13 by 51% and 66%, respectively. In an Eμ-TCL1 mouse model of CLL, ARQ 531 treatment at either 50 or 75mg/kg significantly improved the survival of animals over ibrutinib (25mg/kg) treatment. In a murine model of aggressive lymphoma, ARQ 531 at a dosage of 75mg/kg prolonged survival (median survival = 47 days) compared to ibrutinib-treated (median survival = 38 days) and vehicle-treated (median survival = 35.5 days) groups[1]. | ||
| 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 |
| NCT03162536 | Lymphoma, B-Cell ... 展开 >> Small Lymphocytic Lymphoma Chronic Lymphocytic Leukemia Waldenstrom Macroglobulinemia Mantle Cell Lymphoma Diffuse Large B Cell Lymphoma 收起 << | Phase 1 | Recruiting | April 2019 | United States, Ohio ... 展开 >> Wexner Medical Center at The Ohio State University Recruiting Columbus, Ohio, United States, 43210 Contact 781-994-0300 ClinicalTrials@arqule.com United States, Tennessee Sarah Cannon Research Institute Recruiting Nashville, Tennessee, United States, 37203 Contact 781-994-0300 ClinicalTrials@arqule.com United States, Utah University of Utah, Huntsman Cancer Institute Recruiting Salt Lake City, Utah, United States, 84112 Contact 781-994-0300 ClinicalTrials@arqule.com 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.09mL 0.42mL 0.21mL |
10.44mL 2.09mL 1.04mL |
20.88mL 4.18mL 2.09mL |
| 参考文献 |
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