Home Epigenetics Pim inhibitor Uzansertib (INCB053914) For research use only.

Uzansertib (INCB053914)

Uzansertib (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.

Uzansertib (INCB053914) Chemical Structure

Uzansertib (INCB053914) Chemical Structure

CAS No. 2088852-47-3

Purity & Quality Control

Batch: S880001 DMSO]50 mg/mL]false]]]false]]]false Purity: 99.48%
99.48

Uzansertib (INCB053914) Related Products

Signaling Pathway

Pim Signaling Pathways

Pim Signaling Pathway

Biological Activity

Description Uzansertib (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
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].
Cell Research 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.
In Vivo
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].
Animal Research 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03688152 Completed
Relapsed Diffuse Large B-Cell Lymphoma|Refractory Diffuse Large B-Cell Lymphoma
Incyte Corporation
 December 3 2018 Phase 1

Chemical Information & Solubility

Molecular Weight 611.51 Formula

C26H26F3N5O3.H3O4P
CAS No. 2088852-47-3 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
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DMSO : 50 mg/mL ( (81.76 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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In vivo
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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.

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