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PIM447
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PIM447图片
CAS NO:1210608-43-7
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
LGH447
产品介绍
PIM447 (LGH447) 是一种有效的、口服的、选择性的泛PIM激酶抑制剂,对 PIM1、PIM2 和 PIM3 的Ki值分别为 6、18 和 9 pM。PIM447 具有双重抗肿瘤和骨保护作用。PIM447 诱导细胞凋亡。
生物活性

PIM447 (LGH447) is a potent, orally available, and selective pan-PIMkinaseinhibitor, withKivalues of 6, 18, and 9 pM forPIM1,PIM2, andPIM3, respectively. PIM447 displays dual antimyeloma and bone-protective effects. PIM447 inducesapoptosis[1][2].

体外研究
(In Vitro)

PIM447 (0.05-10 μM; 24-72 hours) shows antiproliferative effect on the multiple myeloma (MM) cells[2].
PIM447 (10 μM; 6-24 hours) induces apoptosis[2].
PIM447 (0.1-10 μM; 48 hours) increases the percentage of cells in the G0-G1 phase and decreases the proliferative phases (S and G2–M) of the cell cycle, in the two cell lines (MM1S and OPM-2 cells) at all doses[2].

Cell Viability Assay[2]

Cell Line:MM1S, MM1R, RPMI-8226, MM144, U266, NCI-H929, OPM-2, RPMI-LR5, U266-Dox4, and U266-LR7 cells
Concentration:0.05, 0.1, 0.5, 1, 5, 10 μM
Incubation Time:24, 48, 72 hours
Result:Sensitive cell lines with IC50 values at 48 hours ranging from 0.2 to 3.3 μM (MM1S, MM1R, RPMI-8226, MM144, U266, and NCI-H929) and less sensitive cell lines with IC50 values at 48 hours >7 μmol/L (OPM-2, RPMI-LR5, U266-Dox4, and U266-LR7).

Western Blot Analysis[2]

Cell Line:MM1S cells
Concentration:10 μM
Incubation Time:6, 12, 24 hours
Result:Promoted the cleavage of initiator caspases, such as caspases 8 and 9, and also the cleavage of the effector caspases 3 and 7, together with PARP cleavage.
体内研究
(In Vivo)

PIM447 (100 mg/kg; p.o.; 5 times for a week) reduces tumor burden[2].

Animal Model:6-week-old female NOD-SCID-IL-2Rγ–/– (NSG) mice (bearing RPMI-8226-luc cells)[2]
Dosage:100 mg/kg
Administration:p.o.; 5 times for a week
Result:Clearly controlled tumor progression as measured by bioluminescence.
Clinical Trial
分子量

440.46

Formula

C24H23F3N4O

CAS 号

1210608-43-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.