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