产品说明书
CEP-40783
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同义名 : | RXDX-106 |
| CAS号 : | 1437321-24-8 | |
| 货号 : | A525104 | |
| 分子式 : | C31H26F2N4O6 | |
| 纯度 : | 99%+ | |
| 分子量 : | 588.558 | |
| MDL号 : | MFCD28502441 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 2 mg/mL(3.4 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 | CEP-40783 is a robust, selective, and orally bioavailable antagonist of AXL and c-Met, exhibiting IC50 values of 7 nM and 12 nM, respectively. In cells transfected with AXL, such as 293GT, CEP-40783's activity is enhanced 27 times more than that of the recombinant enzyme, with an IC50 of 0.26 nM. Additionally, CEP-40783's efficacy against c-Met is pronounced in GTL-16 cells, with an IC50 of 6 nM. This heightened activity in cellular environments may be due to CEP-40783's prolonged binding to AXL and c-Met, aligning with a Type II mechanism. Furthermore, CEP-40783 is highly selective within the kinome, inhibiting over 90% of 298 kinases at a concentration of 1 µM, as indicated by an S90 value of 0.04[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 |
| NCT03454243 | Advanced or Metastatic Solid T... 展开 >>umors 收起 << | Early Phase 1 | Terminated(Sponsor's decision) | - | United States, Texas ... 展开 >> START San Antonio, Texas, United States, 78229 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.70mL 0.34mL 0.17mL |
8.50mL 1.70mL 0.85mL |
16.99mL 3.40mL 1.70mL |
| 参考文献 |
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