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TP-3654 {[allProObj[0].p_purity_real_show]}

货号:A809668

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.

TP-3654 化学结构 CAS号:1361951-15-6
TP-3654 化学结构
CAS号:1361951-15-6
TP-3654 3D分子结构
CAS号:1361951-15-6
TP-3654 化学结构 CAS号:1361951-15-6
TP-3654 3D分子结构 CAS号:1361951-15-6
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TP-3654 纯度/质量文件 产品仅供科研

货号:A809668 标准纯度: {[allProObj[0].p_purity_real_show]}
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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。

TP-3654 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].

TP-3654 动物研究

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
Animal Rats[1]
Dose 40 mg/kg
Administration p.o.
F 0.39
T1/2 4.1 h
Tmax 1 h

TP-3654 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 <<

TP-3654 参考文献

[1]Foulks JM, Carpenter KJ, et al. A small-molecule inhibitor of PIM kinases as a potential treatment for urothelial carcinomas. Neoplasia. 2014 May;16(5):403-12.

TP-3654 实验方案

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

TP-3654 技术信息

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
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