Unesbulin (PTC596)

For research use only.

Catalog No.S8820

1 publication

Unesbulin (PTC596) Chemical Structure

CAS No. 1610964-64-1

Unesbulin (PTC596) is a second-generation BMI-1 inhibitor that accelerates BMI-1 degradation. PTC596 downregulates MCL-1 and induces p53-independent mitochondrial apoptosis. IC50 values at 72 hours ranged from 68 to 340 nM in mantle cell lymphoma (MCL) cell lines.

Selleck's Unesbulin (PTC596) has been cited by 1 publication

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Choose Selective BMI-1 Inhibitors

Biological Activity

Description Unesbulin (PTC596) is a second-generation BMI-1 inhibitor that accelerates BMI-1 degradation. PTC596 downregulates MCL-1 and induces p53-independent mitochondrial apoptosis. IC50 values at 72 hours ranged from 68 to 340 nM in mantle cell lymphoma (MCL) cell lines.
Targets
BMI-1 [1]
()
In vitro

PTC596 induces mitochondrial apoptosis in BMI-1-expressing MCL cells in a p53-independent manner. MCL SP cells were susceptible to PTC596-induced apoptosis[1].

In vivo

PTC596 inhibits myeloid leukemia cell growth in vivo while sparing normal hematopoietic cells[2].

Protocol

Cell Research:

[1]

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  • Cell lines: Z-138 and REC-1 cells
  • Concentrations: 300 nM
  • Incubation Time: 24 h
  • Method:

    Z-138 and REC-1 cells were treated for 24 hours with 300 nM PTC596, after which BCL-2, BCL-XL and MCL-1 protein levels were determined.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: Non-obese diabetic-severe combined immunodeficiency (NOD-SCID)/IL2Rγ-KO (NSG) mice
  • Dosages: 5 mg/kg
  • Administration: by oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 84 mg/mL (199.83 mM)
Water Insoluble
Ethanol '7 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 420.34
Formula
C19H13F5N6
 
CAS No. 1610964-64-1
Storage powder
in solvent
Synonyms N/A
Smiles CC1=NC2=C(N1C3=NC(=C(C(=N3)NC4=CC=C(C=C4)C(F)(F)F)F)N)C=C(C=C2)F

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03761095 Recruiting Drug: PTC596|Drug: Dacarbazine Leiomyosarcoma PTC Therapeutics March 13 2019 Phase 1
NCT03605550 Recruiting Drug: PTC596|Radiation: Radiotherapy High Grade Glioma|Diffuse Intrinsic Pontine Glioma Nationwide Children''s Hospital|PTC Therapeutics August 1 2018 Phase 1

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID