製品番号: HY-19322

PIM447

(別名: LGH447)

8 Cited Publications

カスタマーレビュー

Based on 8 publication(s) in Google Scholar

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.

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純度: 99.52%
CAS 番号: 1210608-43-7
分子式: C₂₄H₂₃F₃N₄O
分子量:440.46

保管条件:

4°C, sealed storage, away from moisture

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

PIM447 構造式

CAS 番号: 1210608-43-7

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価格（税別）

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数量

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (8)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

PIM1

PIM2

PIM3

Pim アイソフォーム固有の製品をすべて表示 :

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: 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]
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]
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]

体外実験

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].

MedChemExpress (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.

体内実験

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

MedChemExpress (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.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 1210608-43-7
性状 Solid
分子量 440.46
分子式 C₂₄H₂₃F₃N₄O
Color White to off-white
SMILES

O=C(C1=CC=C(F)C(C2=C(F)C=CC=C2F)=N1)NC3=C([C@@H]4C[C@H](C)C[C@H](N)C4)C=CN=C3
別名

LGH447
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

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

Publications (8)

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Journal Impact Factor

Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Cell Chem Biol

PIM1 targeted degradation prevents the emergence of chemoresistance in prostate cancer. [Abstract]

2024 Feb 15;31(2):326-337.e11. PMID: 38016478
Blood Adv

Deep PIM kinase substrate profiling reveals new rational co-therapeutic strategies for acute myeloid leukemia. [Abstract]

2024 Aug 13;8(15):3880-3892. PMID: 38739710
Mol Cancer Ther

PIM Kinases Are a Potential Prognostic Biomarker and Therapeutic Target in Neuroblastoma. [Abstract]

2018 Apr;17(4):849-857. PMID: 29440296
J Pathol

Anti-tumour effects of PIM kinase inhibition on progression and chemoresistance of hepatocellular carcinoma. [Abstract]

2020 Sep;252(1):65-76. PMID: 32558942

PIM447 purchased from MedChemExpress. 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.
PLoS One

A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]

2024 Nov 1;19(11):e0308647. PMID: 39485774
bioRxiv

2024 October 24.
bioRxiv

2024 Mar 28.

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (227.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (11.35 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (11.35 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (11.35 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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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 Inhibitor in Clinical Trials for Hematological Malignancies.J Med Chem. 2015 Nov 12;58(21):8373-86. [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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

PIM447

8 Cited Publications

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PIM447

Orally Active Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Apoptosis Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Clinical Compound Library

MedChemExpress（MCE）の使用を引用している文献 PIM447

Pim アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (8)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

PIM447

Orally Active Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Apoptosis Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Clinical Compound Library

MedChemExpress（MCE）の使用を引用している文献 PIM447

Pim アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (8)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

PIM447 関連分類

HY-19322 関連分類