TP-3654 is a selective Pim kinase inhibitor with Ki values of 5nM, 239nM and 42nM for Pim-1, Pim-2 and Pim-3, 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.
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产品名称 | Pim1 ↓ ↑ | Pim2 ↓ ↑ | Pim3 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
SMI-4a |
++
Pim1, IC50: 17 nM |
99%+ | |||||||||||||||||
SGI-1776 free base |
++
Pim1, IC50: 7 nM |
+
Pim2, IC50: 363 nM |
+
Pim3, IC50: 69 nM |
FLT3 | 99+% | ||||||||||||||
AZD-1208 |
+++
Pim1, IC50: 0.4 nM |
+++
Pim2, IC50: 5 nM |
+++
Pim3, IC50: 1.9 nM |
98% | |||||||||||||||
CX-6258 HCl |
+++
Pim1, IC50: 5 nM |
+
Pim2, IC50: 25 nM |
++
Pim3, IC50: 16 nM |
98% | |||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
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]. |
Dose | Rat[1]: 2 mg/kg(i.v.), 40 mg/kg(p.o.), Mice[1] (p.o.): 200mg/kg | ||||||||||||
Administration | i.v., p.o. | ||||||||||||
Pharmacokinetics |
|
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 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.39mL 0.48mL 0.24mL |
11.95mL 2.39mL 1.19mL |
23.90mL 4.78mL 2.39mL |
CAS号 | 1361951-15-6 |
分子式 | C22H25F3N4O |
分子量 | 418.455 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,2-8°C |
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 |
动物实验配方 |