产品说明书
TP-3654
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同义名 : | - |
| CAS号 : | 1361951-15-6 | |
| 货号 : | A809668 | |
| 分子式 : | C22H25F3N4O | |
| 纯度 : | 99%+ | |
| 分子量 : | 418.455 | |
| MDL号 : | MFCD28502206 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,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(119.49 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 | Pim (provirus integration site for Moloney murine leukemia virus) family proteins are highly conserved serine/threonine kinases implicated in transcription, translation, cell cycle, survival, and drug resistance through the numerous targets. TP-3654 is a selective Pim kinase inhibitor with Ki values of 5nM, 239nM and 42nM for Pim-1, Pim-2 and Pim-3 (measured by PIM Kinase), respectively, as well as with an average EC50 of 67nM for cellular PIM-1 inhibition in the PIM-1/BAD overexpression system and with moderate potency to FLT3. Also, cellular study showed that TP-3654 treatment at concentration of 3μM reduced levels of p-BAD in bladder cancer cell line UM-UC-3. TP-3654 could reduce PIM-1–dependent cell growth of T24 with EC50 of 3.54μM and 1.69μM on day 6 and day 10, as well as of UM-UC3 cells with EC50 of 0.82μM and 0.89μM. In vivo study showed that oral dose of 200mg/kg TP-3654 5 days on 2 days off per week for 3 weeks significantly reduced tumor growth of both UM-UC-3 and PC-3 xenograft mice[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 |
| NCT03715504 | Advanced Solid Tumors | Phase 1 | Not yet recruiting | March 2021 | United States, Utah ... 展开 >> Huntsman Cancer Institute Not yet recruiting Salt Lake City, Utah, United States, 84112 Contact: Ignacio Garrido-Laguna, MD, PhD 801-585-0303 Principal Investigator: Ignacio Garrido-Laguna, MD, PhD 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.39mL 0.48mL 0.24mL |
11.95mL 2.39mL 1.19mL |
23.90mL 4.78mL 2.39mL |
| 参考文献 |
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