基本属性 生物活性体外研究体内研究 用途与合成方法 PIM447 DIHYDROCHLORIDE 价格(试剂级) 供应商 供应信息
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PIM447 DIHYDROCHLORIDE

PIM447 DIHYDROCHLORIDE

英文名称:N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide
CAS号:1820565-69-2
分子式:C24H23F3N4O
分子量:440.4608296
EINECS号:
Mol文件:1820565-69-2.mol
PIM447 DIHYDROCHLORIDE 结构式

PIM447 DIHYDROCHLORIDE 性质

储存条件 Store at -20°C
溶解度 水:50.0(最大浓度 mg/mL);97.39(最大浓度 mM)

PIM447 DIHYDROCHLORIDE 用途与合成方法

PIM447 dihydrochloride (LGH447 dihydrochloride) 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 dihydrochloride 具有双重抗肿瘤和骨保护作用。PIM447 dihydrochloride 诱导细胞凋亡。

PIM-447 (0.05-10 µM; 24, 48 and 72 hours)has inhibitory effects in MM cells, it against sensitive cell lines with IC 50 values ranging from 0.2 to 3.3 µM (MM1S, MM1R, RPMI-8226, MM144, U266 and NCI-H929) and less sensitive cell lines with IC 50 values at 48 h >7 µM (OPM-2,RPMI-LR5, U266-Dox4 and U266-LR7).PIM-447 (0.1-10 µM; 24, 48 and 72 hours) does not induce important levels of apoptosis, when PIM447 at 5 µM, it substantially increases annexin-V levels (about 30%) in sensitive cell lines(MM1S, NCI-H929 and RPMI-8226).when PIM447 at 10 µM, 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 (0.1-1 µM) 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 (0.1-1 µM) 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: 0.05-10 µM
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: 0.05-10 µM
Incubation Time: 24, 48 and 72 hours
Result: Induced cell apoptosis at higer doses, had no effects at 0.1-1 uM.

Western Blot Analysis

Cell Line: Sensitive MM cell lines: MM1S, NCI-H929 and RPMI-8226 cells
Concentration: 0.05-10 µM
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 1 µM
Incubation Time: 48 hours
Result: Increased the cleavage of the effector caspases 3 and 7, and the PARP cleavage.

PIM447 (oral gavage; 100 mg/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: 100 mg/kg
Administration: oral gavage; 100 mg/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.

PIM447 DIHYDROCHLORIDE 价格(试剂级)

更新日期 产品编号 产品名称 CAS号 包装 价格
2024-01-25 HY-19322B PIM447 DIHYDROCHLORIDE 1820565-69-2 1mg 1350
2024-01-25 HY-19322B PIM447 DIHYDROCHLORIDE 1820565-69-2 5mg 3000

PIM447 DIHYDROCHLORIDE供应商 更多

上海芮晖化工科技有限公司
现货
联系电话:21-31433387 15618786686
产品介绍:
英文名称:PIM-447 dihydrochloride
CAS:1820565-69-2
纯度:99%
包装信息:0.1g,1g
备注:现货
库存量:>1mg
现货日期:2024/3/27 11:36:30
上海佰世凯化学科技有限公司
联系电话:021-20908456
产品介绍:
英文名称:PIM-447 dihydrochloride
CAS:1820565-69-2
纯度:98% HPLC
包装信息:5mg;10mg;50mg;100mg
备注:Biochemical Reagents; Pharmaceutical Intermediates
上海三牧化工技术有限公司
联系电话:021-38681880 13818891950
产品介绍:
英文名称:N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide
CAS:1820565-69-2
纯度:98%min
包装信息:1mg, 10mg, 100mg, 500mg
备注:1000mg in stock
上海瀚香生物科技有限公司
联系电话:17754423994 17754423994
产品介绍:
英文名称:PIM447 dihydrochloride
CAS:1820565-69-2
纯度:98% HPLC LCMS
包装信息:100mg;500mg;1g;5g
备注:量大优惠,现货促销
北京普西唐生物科技有限公司
联系电话:010-60605840 18892239720
产品介绍:
英文名称:PIM-447 dihydrochloride
CAS:1820565-69-2
纯度:98%
包装信息:1mg;5mg;10mg;50mg

最新发布供应信息

泛PIM抑制剂
上海泽叶生物科技有限公司 2024-03-28