PIM447 (LGH447)

For research use only.

Catalog No.S7985

11 publications

PIM447 (LGH447) Chemical Structure

CAS No. 1210608-43-7(freebase)

PIM447 (LGH447) is a novel pan-PIM kinase inhibitor with Ki values of 6 pM, 18 pM, 9 pM for PIM1, PIM2, PIM3 respectively. It also inhibits GSK3β, PKN1, and PKCτ, but at a significantly lower potency with IC50 between 1 and 5 μM (>105-fold differential relative to the Ki on PIMs). PIM447 induces apoptosis.

Selleck's PIM447 (LGH447) has been cited by 11 publications

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  • (H) MV4-11 cells were treated for 6 hours with or without 3 ng/ml BZM, 10 μM PF, or 3 μM PIM, as indicated, and analyzed.

    Transl Oncol, 2018, 12(2):336-349. PIM447 (LGH447) purchased from Selleck.

Purity & Quality Control

Choose Selective Pim Inhibitors

Biological Activity

Description PIM447 (LGH447) is a novel pan-PIM kinase inhibitor with Ki values of 6 pM, 18 pM, 9 pM for PIM1, PIM2, PIM3 respectively. It also inhibits GSK3β, PKN1, and PKCτ, but at a significantly lower potency with IC50 between 1 and 5 μM (>105-fold differential relative to the Ki on PIMs). PIM447 induces apoptosis.
Targets
Pim1 [1]
(Cell-free assay)
Pim3 [1]
(Cell-free assay)
Pim2 [1]
(Cell-free assay)
6 pM(Ki) 9 pM(Ki) 18 pM(Ki)
In vitro

The kinase selectivity of PIM447 is first determined in biochemical assays for a panel of 68 diverse protein kinases that included PIM2 as well as 9 lipid kinases. In this panel, only PIM2 is significantly inhibited by PIM447 with an IC50 of <0.003 μM, the lowest sensitivity range for the assay. PIM447 also inhibits GSK3β, PKN1, and PKCτ, but at a significantly lower potency with IC50 between 1 and 5 μM (>105-fold differential relative to the Ki on PIMs). The biochemical IC50 for all other kinases tested in this panel is >9 μM. In follow-up cellular assays of GSK3β inhibition, PIM447 is tested up to 20 μM and is not active[1]. PIM447 is cytotoxic for myeloma cells due to cell-cycle disruption and induction of apoptosis mediated by a decrease in phospho-Bad (Ser112) and c-Myc levels and the inhibition of mTORC1 pathway. PIM447 also inhibits in vitro osteoclast formation and resorption, downregulates key molecules involved in these processes, and partially disrupts the F-actin ring, while increasing osteoblast activity and mineralization[2].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MOLM16 MYrBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NVzofWJ4OyCmYYnz MnK1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPT1zNNVYh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IFPlcIxVcXSncj3HcI8h[XO|YYmsJGdKPTB;MD6wNe69VQ>? MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjVyNUi5PEc,OjZ3MEW4PVg9N2F-
KG1 NFSxcIdCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MnnON{Bl[Xm| M{fIcGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1exJINmdGy|IHHmeIVzKDNiZHH5d{BjgSCFZXzsWIl1\XJvR3zvJIF{e2G7LDDHTVUxRTBwMEJOwG0> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjVyNUi5PEc,OjZ3MEW4PVg9N2F-
EOL-1 Mn3qRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NWqxdJk2OyCmYYnz MWDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEWRTD2xJINmdGy|IHHmeIVzKDNiZHH5d{BjgSCFZXzsWIl1\XJvR3zvJIF{e2G7LDDHTVUxRTBwMEJOwG0> NGfVXYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkWwOVg6QCd-Mk[1NFU5QTh:L3G+
M07e NHjQTGtCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MXuzJIRigXN? Mn3LRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPMEflJINmdGy|IHHmeIVzKDNiZHH5d{BjgSCFZXzsWIl1\XJvR3zvJIF{e2G7LDDHTVUxRTBwMEZOwG0> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjVyNUi5PEc,OjZ3MEW4PVg9N2F-
UKE1 NHXwPGNCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M{PXXFMh\GG7cx?= M3TFW2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVVvFNUBk\WyuczDh[pRmeiB|IHThfZMh[nliQ3XscHRqfGW{LVfsc{Bie3OjeTygS2k2OD1yLkC5{txO NHvuTJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkWwOVg6QCd-Mk[1NFU5QTh:L3G+
MV411 NYfUV|ZFSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M132[lMh\GG7cx?= MlLrRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPVkSxNUBk\WyuczDh[pRmeiB|IHThfZMh[nliQ3XscHRqfGW{LVfsc{Bie3OjeTygS2k2OD1yLkGz{txO M3vJS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NUC1PFk5Lz5{NkWwOVg6QDxxYU6=
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SET2 NYL4UIo{SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= Mk\KN{Bl[Xm| NUfwZY15SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTSXQzKGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDD[YxtXGm2ZYKtS4xwKGG|c3H5MEBIUTVyPUCuOFjPxE1? MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjVyNUi5PEc,OjZ3MEW4PVg9N2F-
CMK-11-5 NHvCVJdCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NIrCSGs{KGSjeYO= NYL5[mp{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDUWsuOTFvNTDj[YxteyCjZoTldkA{KGSjeYOgZpkhS2WubGTpeIVzNUeubzDhd5NigSxiR1m1NF0yNjB|zszN NVPvcIJkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1NFU5QThpPkK2OVA2QDl6PD;hQi=>
MOLM13 MYXBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MoXhN{Bl[Xm| M2q4eGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTV;MUVE{KGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDD[YxtXGm2ZYKtS4xwKGG|c3H5MEBIUTVyPUGuN|nPxE1? NUj2UZJWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1NFU5QThpPkK2OVA2QDl6PD;hQi=>
HEL 92.1.7 NEe1PVJCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M33mbVMh\GG7cx?= MYXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiHTDC5Nk4yNjdiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JGNmdGyWaYTldk1IdG9iYYPzZZktKEeLNUC9NU43Ps7:TR?= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjVyNUi5PEc,OjZ3MEW4PVg9N2F-
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OCI-AML5 NUjoR253SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M3T5SFMh\GG7cx?= NHyxUWZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;DTU1CVUx3IHPlcIx{KGGodHXyJFMh\GG7czDifUBE\WyuVHn0[ZIuT2yxIHHzd4F6NCCJSUWwQVEx|ryP NYPLe2x3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1NFU5QThpPkK2OVA2QDl6PD;hQi=>
KG1 NF;tW2VCdnSrdIXtc5Ih[XO|YYm= M{jufVMxKG2pL3vn MVixNUBl[Xm| M33qcmFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvHNUBk\WyuczD4[Y5w\3KjZoTl[EBqdiCvb4Xz[UBie3Onc4Pl[EBieyC2dX3vdkB{fGG|aYOgZZQhOzBibXevb4ctKHCxIIHkJI1m[XO3cnXkJIFnfGW{IEGxJIRigXNicH;zeEB1fW2xcjDpcZBt[W62YYTpc44> M3jGXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NUC1PFk5Lz5{NkWwOVg6QDxxYU6=
KG1 MkizRY51cXS3bX;yJIF{e2G7 NYrm[FBvOzBidH:gNVAxKG2pL3vn MXixNUBl[Xm| NVmxfmVFSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gT2cyKGOnbHzzJJhmdm:pcnHmeIVlKGmwIH3veZNmKGG|c3Xzd4VlKGG|IIT1cY9zKHKnZ4Lld5Nqd25iYYSgN|AhfG9iMUCwJI1oN2upLDDwc{By\CCvZXHzeZJm\CCjZoTldkAyOSCmYYnzJJBwe3RidIXtc5IhcW2ybHHueIF1cW:wIHnuJJBz\XOnbnPlJI9nKDFyMDDt[{9s\yCDcnGtRy=> NGftRnY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkWwOVg6QCd-Mk[1NFU5QTh:L3G+

... Click to View More Cell Line Experimental Data

In vivo Low to moderate in vivo CL is observed for PIM447 across species, as CL values of 20, 28, and 8 mL/min/kg are observed in mouse, rat, and dog, respectively. The volume of distribution is consistently large across species, with Vss of 5.3, 6.4, and 3.6 L/kg observed in mouse, rat, and dog, respectively. Additionally, PIM447 exhibits high oral bioavailability across species, as 84%, 70%, and 71% is observed in mouse, rat, and dog, respectively. The stability of PIM447 in human plasma is high, >90% after a 3 h incubation, and the human plasma protein binding of PIM447 is 95%. With the combination of potent in vitro activity and low to moderate CL, PIM447 demonstrates in vivo target modulation (pS6RP), single agent antitumor activity in a KG-1 AML mouse xenograft model, and druglike properties suitable for development[1]. PIM447 significantly reduces the tumor burden and prevents tumor-associated bone loss in a disseminated murine model of human myeloma[2].

Protocol

Cell Research:

[1]

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  • Cell lines: KG-1 cells
  • Concentrations: 0.05, 0.5, and 5 μM
  • Incubation Time: 2 h
  • Method:

    Following treatment of KG-1 cells with PIM447 for 2 h at the indicated concentrations, cells are lysed in RIPA buffer. Protein concentration is determined using a BCA assay, and 50 μg of lysate is separated by SDS-PAGE using 10% bis-Tris gels. Proteins are transferred onto 0.2 μm nitrocellulose membrane, and pS6RP/total S6RP are detected. Following incubation with secondary antibodies, antibody binding is detected using ECL Advance.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: KG-1 AML xenograft mouse model 
  • Dosages: 30 or 100 mg/kg
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 88 mg/mL (184.51 mM)
Water Insoluble
Ethanol '88 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 476.92
Formula

C24H23F3N4O.HCl

CAS No. 1210608-43-7(freebase)
Storage powder
in solvent
Synonyms N/A
Smiles CC1CC(CC(C1)N)C2=C(C=NC=C2)NC(=O)C3=NC(=C(C=C3)F)C4=C(C=CC=C4F)F

In vivo Formulation Calculator (Clear solution)

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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

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  • Computed Result

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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02160951 Completed Drug: LGH447 Multiple Myeloma Novartis Pharmaceuticals|Novartis September 2014 Phase 1
NCT02078609 Completed Drug: LGH447|Drug: LGH447 + midostaurin AML and High Risk MDS Novartis Pharmaceuticals|Novartis March 20 2014 Phase 1
NCT01456689 Completed Drug: LGH447|Drug: midazolam Multiple Myeloma Novartis Pharmaceuticals|Novartis April 25 2012 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Pim Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID