INCB053914

For research use only.

Catalog No.S8800

2 publications

INCB053914 Chemical Structure

CAS No. 2088852-47-3

INCB053914 is a novel, ATP-competitive, small molecule, pan-inhibitor of PIM kinases with IC50 values of 0.24 nM, 30 nM and 0.12 nM for PIM1, PIM2 and PIM3 respectively in biochemical assays.

Selleck's INCB053914 has been cited by 2 publications

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Biological Activity

Description INCB053914 is a novel, ATP-competitive, small molecule, pan-inhibitor of PIM kinases with IC50 values of 0.24 nM, 30 nM and 0.12 nM for PIM1, PIM2 and PIM3 respectively in biochemical assays.
In vitro

INCB053914 potently inhibits the activities of all three PIM isozymes with half maximal inhibitory concentration (IC50) values in the order of PIM1 ≈ PIM3 < PIM2. It is highly selective against a panel of more than 50 kinases (>475-fold selectivity), except for RSK2 for which INCB053914 has modest potency (IC50 = 7.1 μM). No kinase other than Per-Arnt-Sim (PAS) kinase is significantly inhibited by INCB053914 (100 nM)[1]. In cell proliferation assays, INCB053914 is active as a single agent in the majority of cell lines derived from different hematological malignancies, including MM, AML, DLBCL, MCL and T-ALL, with IC50 values ranging from 3-300 nM. INCB053914 synergizes with a variety of cytotoxic and targeted agents, reducing the viability of a panel of hematological tumor cell lines[2].

In vivo

In vivo, single-agent INCB053914 inhibits Bcl-2-associated death promoter protein phosphorylation and dose-dependently inhibited tumor growth in acute myeloid leukemia and multiple myeloma xenografts[2]. INCB053914 inhibits tumor growth in a dose-dependent manner in mice bearing MOLM-16 (AML) or KMS-12-BM (MM) tumors. A pharmacokinetic analysis of INCB053914 plasma concentrations up to 16 hours post oral administration in MOLM-16 and KMS-12-BM tumor-bearing mice suggests dose proportionality[1].

Protocol

Cell Research:

[1]

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  • Cell lines: MOLM-16 (AML), Pfeiffer (DLBCL), KMS-12-PE (MM), and KMS-12-BM (MM) cells
  • Concentrations: 0-1 μM
  • Incubation Time: 2 h
  • Method:

    106 MOLM-16 (AML), Pfeiffer (DLBCL), KMS-12-PE (MM), and KMS-12-BM (MM) cells are incubated with INCB053914 at concentrations ranging from 0 (phosphate-buffered saline [PBS]) to 1 μM for 2 hours in RPMI medium. Cells are centrifuged at 1,000 rpm for 10 minutes and lysed with 1× lysis buffer supplemented with 1 mM phenylmethane sulfonyl fluoride and proteinase inhibitor cocktail. Cell lysates are stored at -80°C before determining phosphoprotein and PIM2 levels by Western blotting.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Human MOLM-16 (AML) and KMS-12-BM (MM) xenografts established in SCID mice
  • Dosages: 0-100 mg/kg
  • Administration: by oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 50 mg/mL (81.76 mM)

* 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 611.51
Formula

C26H26F3N5O3.H3O4P

CAS No. 2088852-47-3
Storage powder
in solvent
Synonyms N/A
Smiles CC1CN(CC(C1O)N)C2=C3CCC(C3=NC=C2NC(=O)C4=NC(=C(C=C4)F)C5=C(C=CC=C5F)F)O.OP(=O)(O)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03688152 Completed Drug: INCB053914|Drug: INCB050465 Relapsed Diffuse Large B-Cell Lymphoma|Refractory Diffuse Large B-Cell Lymphoma Incyte Corporation December 3 2018 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

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Pim Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID