PIM447 (Synonyms: LGH447)

目录号: HY-19322 纯度: 99.52%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

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。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PIM447 Chemical Structure

CAS No. : 1210608-43-7

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3. 试用装只面向终端客户。

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥2907	In-stock
1 mg	￥1363	In-stock
5 mg	￥3000	In-stock
10 mg	￥4800	In-stock
50 mg		询价
100 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of PIM447:

(1S,3R,5R)-PIM447 dihydrochloride In-stock
PIM-447 dihydrochloride In-stock
PIM447 hydrochloride 询价

MCE 顾客使用本产品发表的 5 篇科研文献

: PIM447 purchased from MCE. Usage Cited in: J Pathol. 2020 Sep;252(1):65-76. [Abstract]; The alteration of MAPK/ERK pathway is validated by Western blotting with tumour lysates from the animal model, as illustrated by a downregulation of pERK1/2 in the PIM447 treatment group.

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PIM1 PIM2 PIM3

生物活性
纯度 & 产品资料
参考文献

生物活性

PIM447 (LGH447) is a potent, orally available, and selective pan-PIM kinase inhibitor, with K_i values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 displays dual antimyeloma and bone-protective effects. PIM447 induces apoptosis^[1]^[2].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
CMK	GI₅₀	0.28 μM Compound: 8; PIM447	Antiproliferative activity against human CMK cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human CMK cells after 3 days by CellTiter-Glo assay	[PMID: 26505898]
EOL1	GI₅₀	0.01 μM Compound: 8; PIM447	Antiproliferative activity against human EOL-1 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human EOL-1 cells after 3 days by CellTiter-Glo assay	[PMID: 26505898]
HEL 92.1.7	GI₅₀	1.66 μM Compound: 8; PIM447	Antiproliferative activity against human HEL 92.1.7 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human HEL 92.1.7 cells after 3 days by CellTiter-Glo assay	[PMID: 26505898]
KG-1	GI₅₀	0.01 μM Compound: 8; PIM447	Antiproliferative activity against human KG1 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human KG1 cells after 3 days by CellTiter-Glo assay	[PMID: 26505898]
KMS-11	EC₅₀	0.17 μM Compound: 2	Antiproliferative activity against human KMS-11 cells expressing firefly luciferase assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo assay Antiproliferative activity against human KMS-11 cells expressing firefly luciferase assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo assay	[PMID: 33258605]
KMS-11	EC₅₀	0.17 μM Compound: 8; PIM447	Antiproliferative activity against luciferase expressing human KMS11 cells after 72 hrs by Cell-TiterGlo assay Antiproliferative activity against luciferase expressing human KMS11 cells after 72 hrs by Cell-TiterGlo assay	[PMID: 26505898]
KMS-11	EC₅₀	0.17 μM Compound: 1c; PIM447	Antiproliferative activity against human KMS11 expressing luciferase gene after 72 hrs by cell titer glo-based cell viability assay Antiproliferative activity against human KMS11 expressing luciferase gene after 72 hrs by cell titer glo-based cell viability assay	[PMID: 26995528]
MOLM-13	GI₅₀	1.39 μM Compound: 8; PIM447	Antiproliferative activity against human MOLM13 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human MOLM13 cells after 3 days by CellTiter-Glo assay	[PMID: 26505898]
MV4-11	GI₅₀	0.13 μM Compound: 8; PIM447	Antiproliferative activity against human MV411 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human MV411 cells after 3 days by CellTiter-Glo assay	[PMID: 26505898]
NB-4	GI₅₀	7 μM Compound: 8; PIM447	Antiproliferative activity against human NB4 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human NB4 cells after 3 days by CellTiter-Glo assay	[PMID: 26505898]
NOMO-1	GI₅₀	10 μM Compound: 8; PIM447	Antiproliferative activity against human NOMO1 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human NOMO1 cells after 3 days by CellTiter-Glo assay	[PMID: 26505898]
OCI-AML2	GI₅₀	5.53 μM Compound: 8; PIM447	Antiproliferative activity against human OCI-AML2 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human OCI-AML2 cells after 3 days by CellTiter-Glo assay	[PMID: 26505898]
OCI-AML-3	GI₅₀	2.92 μM Compound: 8; PIM447	Antiproliferative activity against human OCI-AML3 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human OCI-AML3 cells after 3 days by CellTiter-Glo assay	[PMID: 26505898]
OCI-AML-5	GI₅₀	10 μM Compound: 8; PIM447	Antiproliferative activity against human OCI-AML5 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human OCI-AML5 cells after 3 days by CellTiter-Glo assay	[PMID: 26505898]
P31-FUJ	GI₅₀	5.06 μM Compound: 8; PIM447	Antiproliferative activity against human P31/FUJ cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human P31/FUJ cells after 3 days by CellTiter-Glo assay	[PMID: 26505898]
SET-2	GI₅₀	0.48 μM Compound: 8; PIM447	Antiproliferative activity against human SET2 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human SET2 cells after 3 days by CellTiter-Glo assay	[PMID: 26505898]
SIG-M5	GI₅₀	8.66 μM Compound: 8; PIM447	Antiproliferative activity against human SIG-M5 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human SIG-M5 cells after 3 days by CellTiter-Glo assay	[PMID: 26505898]
SKM-1	GI₅₀	2.69 μM Compound: 8; PIM447	Antiproliferative activity against human SKM1 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human SKM1 cells after 3 days by CellTiter-Glo assay	[PMID: 26505898]
TF-1	GI₅₀	1.96 μM Compound: 8; PIM447	Antiproliferative activity against human TF1 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human TF1 cells after 3 days by CellTiter-Glo assay	[PMID: 26505898]
THP-1	GI₅₀	5.31 μM Compound: 8; PIM447	Antiproliferative activity against human THP1 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human THP1 cells after 3 days by CellTiter-Glo assay	[PMID: 26505898]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (227.04 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2704 mL	11.3518 mL	22.7035 mL
5 mM	0.4541 mL	2.2704 mL	4.5407 mL
10 mM	0.2270 mL	1.1352 mL	2.2704 mL

查看完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (11.35 mM); 澄清溶液

此方案可获得 ≥ 5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (11.35 mM); 澄清溶液

此方案可获得 ≥ 5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (11.35 mM); 澄清溶液

此方案可获得 ≥ 5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.52%

选择批次：

Data Sheet (630 KB) SDS (252 KB)

COA (290 KB) HNMR (141 KB) RP-HPLC (169 KB) LCMS (356 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Burger MT, et al. Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibito [Content Brief]

[2]. Paíno T et al. The novel pan-PIM kinase inhibitor, PIM447, displays dual anti-myeloma and bone protective effects, and potently synergizes with current standards of care. Clin Cancer Res. 2016 Jul 20. [Content Brief]

[3]. Peters TL et al. Control of translational activation by PIM kinase in activated B-cell diffuse large B-cell lymphoma confers sensitivity to inhibition by PIM447. Oncotarget. 2016 Aug 20 [Content Brief]

PIM447 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2704 mL	11.3518 mL	22.7035 mL	56.7588 mL
	5 mM	0.4541 mL	2.2704 mL	4.5407 mL	11.3518 mL
	10 mM	0.2270 mL	1.1352 mL	2.2704 mL	5.6759 mL
	15 mM	0.1514 mL	0.7568 mL	1.5136 mL	3.7839 mL
	20 mM	0.1135 mL	0.5676 mL	1.1352 mL	2.8379 mL
	25 mM	0.0908 mL	0.4541 mL	0.9081 mL	2.2704 mL
	30 mM	0.0757 mL	0.3784 mL	0.7568 mL	1.8920 mL
	40 mM	0.0568 mL	0.2838 mL	0.5676 mL	1.4190 mL
	50 mM	0.0454 mL	0.2270 mL	0.4541 mL	1.1352 mL
	60 mM	0.0378 mL	0.1892 mL	0.3784 mL	0.9460 mL
	80 mM	0.0284 mL	0.1419 mL	0.2838 mL	0.7095 mL
	100 mM	0.0227 mL	0.1135 mL	0.2270 mL	0.5676 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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PIM447 (Synonyms: LGH447)

Customer Review

Other Forms of PIM447:

MCE 顾客使用本产品发表的 5 篇科研文献

PIM447 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Pim 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

PIM447 相关分类

完整储备液配制表

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PIM447 (Synonyms: LGH447)

Customer Review

Other Forms of PIM447:

PIM447 相关抗体

MCE 顾客使用本产品发表的 5 篇科研文献

PIM447 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Pim 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

PIM447 相关抗体:

摩尔计算器

稀释计算器

PIM447 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

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