Home Epigenetics Pim inhibitor Uzansertib (INCB053914)

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Uzansertib (INCB053914) Pim inhibitor

Cat.No.S8800

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) Pim inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 611.51

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Quality Control

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

Solubility

In vitro
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DMSO : 50 mg/mL (81.76 mM)
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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 611.51 Formula

C26H26F3N5O3.H3O4P

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

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

Mechanism of Action

In vitro

Uzansertib (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 this compound has modest potency (IC50 = 7.1 μM). No kinase other than Per-Arnt-Sim (PAS) kinase is significantly inhibited by INCB053914 (100 nM). In cell proliferation assays, it 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. This compound synergizes with a variety of cytotoxic and targeted agents, reducing the viability of a panel of hematological tumor cell lines.
In vivo

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

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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