T-3775440 HCl

Catalog No.S8438 Batch:S843801

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Technical Data

Formula

C18H23ClN4O
Molecular Weight 346.85 CAS No. 1422535-52-1
Solubility (25°C)* In vitro DMSO 69 mg/mL (198.93 mM)
Water 22 mg/mL (63.42 mM)
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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].
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 (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[2]
  • 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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.