T-3775440 HCl

For research use only.

Catalog No.S8438

T-3775440 HCl Chemical Structure

CAS No. 1422535-52-1

T-3775440 HCl is an irreversible LSD1 inhibitor that is highly selective for LSD1 relative to other monoamine oxidases (e.g., MAO-A and MAO-B), with an IC50 value of 2.1 nmol/L.

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Biological Activity

Description T-3775440 HCl is an irreversible LSD1 inhibitor that is highly selective for LSD1 relative to other monoamine oxidases (e.g., MAO-A and MAO-B), with an IC50 value of 2.1 nmol/L.
Targets
LSD1 [1]
()
2.1 nM
In vitro

T-3775440 treatment enforces transdifferentiation of erythroid/megakaryocytic lineages into granulomonocytic-like lineage cells. T-3775440 disrupts the interaction between LSD1 and growth factor-independent 1B (GFI1B), a transcription factor critical for the differentiation processes of erythroid and megakaryocytic lineage cells. 48-hour T-3775440 treatment induces cell-cycle arrest and apoptosis in AEL (TF-1a, HEL92.1.7) and AMKL cell lines (CMK11-5, M07e). T-3775440 treatment increases the G1 and sub-G1 phase populations in TF-1a and CMK11-5 cells[1].

Assay
Methods Test Index PMID
Western blot
p27 / cPARP ; 

PubMed: 27903753     


TF-1a and CMK11-5 cells were treated with the indicated concentration of T-3775440 for 24 or 48 hours. Treated cells were subsequently harvested and lysed to prepare total lysates. Immunoblotting analyses were performed to determine the expression levels of p27, cleaved PARP, and β-actin in the cell lysates.

27903753
Growth inhibition assay
IC50; 

PubMed: 27903753     


In vitro proliferation assay of 27 leukemia cell lines. Cells were treated with T-3775440 for 3 days. Red bars, AEL cell lines; green bars, AMKL cell lines; and blue bars, T-ALL cell lines.

27903753
In vivo

T-3775440 exerts tumor growth suppression in in vivo mouse xenograft models of AML. In mice, T-3775440 treatment results in a transient reduction in platelets, followed by a significant rebound. There is no obvious effect on red blood cell counts following a single administration. T-3775440 also exhibits potent antitumor effects in an additional AEL model of HEL 92.1.7 and an AMKL model of CMK11-5, possessing profound anti-AEL and anti-AMKL activity[1].

Protocol

Cell Research:

[1]

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  • Cell lines: TF-1a and CMK11-5 cells
  • Concentrations: 0, 10, 50 nM (TF-1a cells); 0, 20, 100 nM (CMK11-5 cells)
  • Incubation Time: 24 and 48 h
  • Method:

    TF-1a and CMK11-5 cells are treated with the indicated concentration of T-3775440 for 24 or 48 hours. Treated cells are subsequently harvested and lysed to prepare total lysates. Immunoblotting analyses are performed to determine the expression levels of p27, cleaved PARP, and β-actin in the cell lysates.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: Female C.B17/Icr-scid/scid Jcl mice subcutaneously (s.c.) inoculated in the flank with AML cells
  • Dosages: 15-20 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 69 mg/mL (198.93 mM)
Water 22 mg/mL (63.42 mM)
Ethanol Insoluble

* 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 346.85
Formula

C18H23ClN4O

CAS No. 1422535-52-1
Storage powder
in solvent
Synonyms N/A
Smiles CN1C=C(C=N1)C(=O)NC2=CC=C(C=C2)C3CC3NCC4CC4.Cl

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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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID