PIM447 (Synonyms: LGH447)

Name: PIM447
Brand: MedChemExpress
SKU: HY-19322
Rating: 5.0 (7 reviews)

Cat. No.: HY-19322 Purity: 99.52%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

PIM447 Chemical Structure

CAS No. : 1210608-43-7

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of PIM447:

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

6 Publications Citing Use of MCE PIM447

: 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.

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PIM1 PIM2 PIM3

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

PIM1

PIM2

PIM3

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]

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].

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.

In Vivo

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.

Clinical Trial

Molecular Weight

440.46

Formula

C₂₄H₂₃F₃N₄O

CAS No.

1210608-43-7

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.52%

Select Batch:

Data Sheet (282 KB) SDS (252 KB)

COA (253 KB) HNMR (141 KB) RP-HPLC (169 KB) LCMS (356 KB)

Handling Instructions (2659 KB)

References

[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]

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 Related Classifications

Help & FAQs

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PIM447 (Synonyms: LGH447)

Customer Review

Other Forms of PIM447:

6 Publications Citing Use of MCE PIM447

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•Related Small Molecules:

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Purity & Documentation

References

Customer Review

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Complete Stock Solution Preparation Table

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PIM447 (Synonyms: LGH447)

Customer Review

Other Forms of PIM447:

PIM447 Related Antibodies

6 Publications Citing Use of MCE PIM447

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Pim Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

PIM447 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

PIM447 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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