PIM447

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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。

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K_i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, withK_ivalues 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.