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PIM447 {[allProObj[0].p_purity_real_show]}

货号:A735192 同义名: LGH447

PIM-447 is pan-PIM kinase inhibitor, including Moloney Murine Leukemia (PIM)1, 2, and 3 Kinase.

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
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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]}
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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 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 440.461
别名 LGH447
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,Store in freezer, under -20°C

溶解度
动物实验配方
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