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细胞凋亡 表观遗传学 JAK-STAT-Signaling 帕金森与阿尔茨海默症 肿瘤表观遗传和基因调控 细胞死亡
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/ PIM447

PIM447 {[allProObj[0].p_purity_real_show]}

货号：A735192 同义名： LGH447

PIM447是一种泛 PIM 激酶抑制剂，能够抑制包括莫隆小鼠白血病（PIM）1、2 和 3 激酶在内的 PIM 激酶。

PIM447 化学结构 CAS号：1210608-43-7
PIM447 化学结构
CAS号：1210608-43-7
PIM447 3D分子结构
CAS号：1210608-43-7
PIM447 化学结构 CAS号：1210608-43-7
PIM447 3D分子结构 CAS号：1210608-43-7
规格 价格 会员价 库存 数量
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PIM447 纯度/质量文件 产品仅供科研

货号：A735192 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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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。

PIM447 生物活性

描述 PIM447 (LGH447) is a strong, orally administered, and specific inhibitor targeting all PIM kinases, exhibiting Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 offers both anti-myeloma and bone-protection benefits, and it triggers apoptosis[1].[2].
体内研究

Administering PIM447 (100 mg/kg; orally; five times weekly) reduces the tumor load[2].
体外研究

When applied to multiple myeloma (MM) cells, PIM447 (0.05-10 μM; over 24-72 hours) inhibits cell proliferation[2].

PIM447, at a concentration of 10 μM for durations ranging from 6 to 24 hours, initiates cell apoptosis[2].

PIM447, within a concentration range of 0.1-10 μM over 48 hours, raises the percentage of cells in the G0-G1 phase while reducing those in the S and G2-M proliferative phases across all doses, affecting both MM1S and OPM-2 cell lines[2].

PIM447 细胞实验

Cell Line
Concentration Treated Time Description References
COA67 cells 7.5 μM 8 hours PIM447 significantly increased apoptosis in COA67 cells. J Pediatr Surg. 2021 Jun;56(6):1157-1164.
NCI-H929 200 nM 72 hours Evaluate the synergistic effect of PIM447 in combination with pomalidomide and dexamethasone, results showed a significant increase in the percentage of apoptotic cells Cancers (Basel). 2020 Sep 24;12(10):2743.
RPMI-8226 100 nM 72 hours Evaluate the synergistic effect of PIM447 in combination with pomalidomide and dexamethasone, results showed a significant increase in the percentage of apoptotic cells Cancers (Basel). 2020 Sep 24;12(10):2743.
MM.1S 100 nM 72 hours Evaluate the synergistic effect of PIM447 in combination with pomalidomide and dexamethasone, results showed a significant increase in the percentage of apoptotic cells Cancers (Basel). 2020 Sep 24;12(10):2743.
HuH6 cells 7.5 μM 72 hours PIM447 significantly increased apoptosis in HuH6 cells. J Pediatr Surg. 2021 Jun;56(6):1157-1164.
MV4-11 cells 2 μM 48 hours PIM447 remarkably enhanced bortezomib-induced apoptosis Transl Oncol. 2019 Feb;12(2):336-349.
COA67 cells 5 μM 24 hours PIM447 significantly decreased the migration and invasion of COA67 cells. J Pediatr Surg. 2021 Jun;56(6):1157-1164.
HuH6 cells 5 μM 24 hours PIM447 significantly decreased the migration and invasion of HuH6 cells. J Pediatr Surg. 2021 Jun;56(6):1157-1164.
COA67 cells 0–20 μM 72 hours PIM447 significantly decreased the viability and proliferation of COA67 cells. J Pediatr Surg. 2021 Jun;56(6):1157-1164.
HuH6 cells 0–12 μM 72 hours PIM447 significantly decreased the viability and proliferation of HuH6 cells. J Pediatr Surg. 2021 Jun;56(6):1157-1164.
Ba/F3 cells 10 µM, 1 µM, 0.1 µM 96 hours Evaluate the effect of PIM447 on the growth and viability of Ba/F3 cells, showing that PIM447 significantly reduces the growth and viability of cells dependent on JAK/STAT pathway mutations. NPJ Precis Oncol. 2024 Jul 20;8(1):152.
M07e cells 10 µM, 1 µM, 0.1 µM 96 hours Evaluate the effect of PIM447 on the growth and viability of M07e cells, showing that PIM447 significantly reduces the growth and viability of cells dependent on JAK/STAT pathway mutations. NPJ Precis Oncol. 2024 Jul 20;8(1):152.
Jurkat cells 10 µM, 1 µM, 0.1 µM 96 hours Evaluate the effect of PIM447 on the growth and viability of Jurkat cells, showing that PIM447 significantly reduces the growth and viability of cells dependent on JAK/STAT pathway mutations. NPJ Precis Oncol. 2024 Jul 20;8(1):152.
UKE-1 cells 300nM 72 hours To assess the effect of PIM447 on pBAD levels, results showed that PIM447 significantly reduced pBAD levels, indicating its on-target effect. Clin Cancer Res. 2021 Jun 15;27(12):3456-3468.

PIM447 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice JAK2V617F-mutant MPN model Oral gavage 12.5mg/kg Daily for 7 weeks To evaluate the effect of PIM447 in combination with ruxolitinib and LEE011, results showed that the combination therapy significantly reduced spleen and liver size, improved bone marrow fibrosis, and prolonged survival. Clin Cancer Res. 2021 Jun 15;27(12):3456-3468.
CB17-SCID mice Human plasmacytoma model Oral and intraperitoneal injection 50 mg/kg 5 times per week, continuous treatment Evaluate the in vivo antitumor effect of PIM447 in combination with pomalidomide and dexamethasone, results showed significant delay in tumor growth and prolonged survival of treated mice Cancers (Basel). 2020 Sep 24;12(10):2743.

PIM447 参考文献

[1]Burger MT, et al. Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibito

[2]Paíno T et al. The novel pan-PIM kinase inhibitor, PIM447, displays dual anti-myeloma and bone protective effects, and potently synergizes with current standards of care. Clin Cancer Res. 2016 Jul 20.

PIM447 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.27mL

0.45mL

0.23mL

11.35mL

2.27mL

1.14mL

22.70mL

4.54mL

2.27mL

PIM447 技术信息

CAS号1210608-43-7
分子式C24H23F3N4O
分子量 440.46
SMILES Code O=C(NC1=C([C@H]2C[C@@H](N)C[C@@H](C)C2)C=CN=C1)C3=NC(C4=C(F)C=CC=C4F)=C(F)C=C3
MDL No. MFCD30489724
别名 LGH447
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C
溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

Tags: PIM447 | 1210608-43-7 | LGH447 | PIM 447 | PIM-447 | LGH 447 | LGH-447 | PIM Kinase Inhibitor | JAK/STAT Signaling | Apoptosis | Pim | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | PIM447 纯度/质量文件 | PIM447 亚型比较 | PIM447 生物活性 | PIM447 参考文献 | PIM447 实验方案 | PIM447 技术信息

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