Atuveciclib Racemate
产品说明书
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同义名 : | BAY-1143572 Racemate;Atuveciclib;BAY-1143572 |
| CAS号 : | 1414943-88-6 | |
| 货号 : | A908334 | |
| 分子式 : | C18H18FN5O2S | |
| 纯度 : | 99%+ | |
| 分子量 : | 387.431 | |
| MDL号 : | MFCD30502894 | |
| 存储条件： |
Pure form Keep in dark place,Sealed in dry,2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(271.02 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 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Atuveciclib (BAY-1143572) suppresses the growth of seven AML cell lines, both with and without MLL rearrangements, displaying a median IC50 value of 385 nM (ranging from 230 to 1100 nM) and triggers apoptosis[1]. Atuveciclib (BAY-1143572) exhibits potent and highly selective inhibitory activity against PTEFb/CDK9 kinase within the low nanomolar range, with a selectivity that is at least 50 times greater against other CDKs. It also demonstrates favorable selectivity over a range of non-CDK kinases and broad antiproliferative effects across various tumor cell lines, achieving sub-micromolar IC50 values. A concentration-dependent decrease in the phosphorylation of RNA polymerase II, along with subsequent reductions in MYC mRNA and protein levels, has been observed[2]. | ||
| 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 |
| NCT02345382 | Leukemia | Phase 1 | Completed | - | United States, Massachusetts ... 展开 >> Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02215 United States, New Jersey Hackensack University Medical Center Hackensack, New Jersey, United States, 07601 United States, New York Columbia University Medical Center New York, New York, United States, 10032 United States, South Carolina Medical University of South Carolina Charleston, South Carolina, United States, 29425 United States, Tennessee Vanderbilt University Medical Center Nashville, Tennessee, United States, 37232 Germany Universitätsklinikum der Johann Wolfgang Goethe Universität Frankfurt, Hessen, Germany, 60596 Medizinische Fakultät Carl Gustav Carus Dresden, Sachsen, Germany, 01307 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.58mL 0.52mL 0.26mL |
12.91mL 2.58mL 1.29mL |
25.81mL 5.16mL 2.58mL |
| 参考文献 |
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