PIM-447 dihydrochloride - CAS:1820565-69-2 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	PIM-447 dihydrochloride
英文名称:	PIM-447 dihydrochloride
别名:	LGH447 dihydrochloride
CAS No:	1820565-69-2	分子式:	C₂₄H₂₅Cl₂F₃N₄O	分子量:	513.38
CAS No:	1820565-69-2
分子式:	C₂₄H₂₅Cl₂F₃N₄O
分子量:	513.38

安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)

P10799 PIM-447 dihydrochloride ≥98% (psaitong)

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包装规格：

1mg 5mg 10mg 50mg in glass bottle

溶解性：

溶于DMSO（≥ 46.7 mg/mL）

产品描述：

基本信息

产品编号：	P10799
产品名称：	PIM-447 dihydrochloride
CAS:	1820565-69-2	储存条件	粉末	-20℃	四年

分子式：	C24H25Cl2F3N4O		溶于液体	-80℃	6个月
分子量：	513.38			-20℃	1个月
化学名：	2-Pyridinecarboxamide,N-[4-[(1R,3S,5S)-3-amino-5-methylcyclohexyl]-3-pyridinyl]-6-(2,6-difluorophenyl)-5-fluoro-,hydrochloride (1:2)
Solubility (25°C)：
体外:	DMSO
	Ethanol
	Water
体内(现配现用):
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	1.9479mL	9.7394mL	19.4787mL
5mM	0.3896mL	1.9479mL	3.8957mL
10mM	0.1948mL	0.9739mL	1.9479mL

生物活性

产品描述	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9pM。
靶点	Ki:6pM (PIM1);18pM (PIM1);9pM (PIM3)
体外研究	PIM-447 (0.05-10µM;24,48 and 72 hours) has inhibitory effects in MM cells,it against sensitive cell lines with IC50 values ranging from 0.2 to 3.3µM (MM1S,MM1R,RPMI-8226,MM144,U266 and NCI-H929) and less sensitive cell lines with IC50 values at 48h>7µM (OPM-2,RPMI-LR5,U266-Dox4 and U266-LR7).PIM-447 (0.1-10µM;24,48 and 72 hours) does not induce important levels of apoptosis,when PIM447 at 5µM,it substantially increases annexin-V levels (about 30%) in sensitive cell lines(MM1S,NCI-H929 and RPMI-8226).When PIM447 at 10µM,it induces apoptosis in all the cell lines but to a lesser extent in OPM-2 and RPMI-LR5.PIM447 promotes the cleavage of initiator caspases,such as caspases 8 and 9,and increases the cleavage of the effector caspases 3 and 7,together with PARP cleavage in MM1S,RPMI-8226 and NCI-H929 cells.PIM447 (0.1-1µM) increases the percentage of cells in the G0/G1 phase and decreases the proliferative phases (S and G2/M) of the cell cycle.The effects at low concentrations (0.1-1µM) were more pronounced in MM1S cells than in OPM-2. Cell Viability Assay
	Cell Line:	Sensitive MM cell lines:MM1S,MM1R,RPMI-8226,MM144,U266 and NCI-H929 cells Less sensitive MM cell lines:OPM-2,RPMI-LR5,U266-Dox4 and U266-LR7cells
	Concentration:	0.05-10µM
	Incubation Time:	24,48 and 72 hours
	Result:	Was cytotoxic for MM cells (PIM kinases highly expressed).
	Apoptosis Analysis
	Cell Line:	Sensitive MM cell lines:MM1S,NCI-H929 and RPMI-8226 cells Less sensitive MM cell lines:OPM-2 and RPMI-LR5 cells
	Concentration:	0.05-10µM
	Incubation Time:	24,48 and 72 hours
	Result:	Induced cell apoptosis at higer doses, had no effects at 0.1-1uM.
	Western Blot Analysis
	Cell Line:	Sensitive MM cell lines:MM1S,NCI-H929 and RPMI-8226 cells
	Concentration:	0.05-10µM
	Incubation Time:	24, 48 hours
	Result:	Increased the cleavage of the effector caspases 3 and 7,and the PARP cleavage.
	Cell Cycle Analysis
	Cell Line:	MM1S,OPM-2 cells
	Concentration:	0.1,0.5 or 1µM
	Incubation Time:	48 hours
	Result:	Increased the cleavage of the effector caspases 3 and 7,and the PARP cleavage.
体内研究	PIM447 (oral gavage;100mg/kg;5 times/week) clearly controlls tumor progression and the serum levels of hIgλ secreted by RPMI-8226-luc cells in mouse model of bone marrow-disseminated human multiple myeloma.
	Animal Model:	RPMI-8226-luc cells are injected intravenously into 6-week-old female NODSCID-IL-2Rγ-/-(NSG) mice.
	Dosage:	100mg/kg
	Administration:	oral gavage;100mg/kg;5 times/week
	Result:	Was well tolerated,as the body weight of mice did not decrease by more than 10%.Increased bone volume density and trabecular number and reduced trabecular separation relative to vehicle group.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

质量 =

浓度 *

体积 *

分子量

*选择对应的单位 *空出希望得到的变量，填写另外两个变量

用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入输出 )

* = *

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

摩尔浓度计算公式

稀释公式

连续稀释计算器方程

连续稀释

计算结果