DT-061 (SMAP)

Catalog No.S8774

For research use only.

DT-061 (SMAP) is a bioavailable PP2A activator. It decreases cell viability in HCC827 and HCC3255 cell lines, with IC50 values of 14.3 μM and 12.4 μM respectively.

DT-061 (SMAP) Chemical Structure

CAS No. 1809427-19-7

Selleck's DT-061 (SMAP) has been cited by 2 Publications

Purity & Quality Control

Choose Selective PP2A Inhibitors

Biological Activity

Description DT-061 (SMAP) is a bioavailable PP2A activator. It decreases cell viability in HCC827 and HCC3255 cell lines, with IC50 values of 14.3 μM and 12.4 μM respectively.
Targets
PP2A [1]
Assay
Methods Test Index PMID
Western blot Cleaved PARP ; p-EGFR / EGFR / p-ERK / ERK / p-AKT / AKT 30830869
In vivo

PP2A reactivation using single agent SMAP DT-061 is a well-tolerated and orally bioavailable therapeutic strategy that is as efficacious as a combination of kinase inhibitors in antagonizing EGFR-driven TKI-resistant LUAD models. Furthermore, treatment with SMAP can overcome resistance in those models, with an even greater effect when combined with afatinib[1].

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: HCC827 and H3255 cell lines
  • Concentrations: 2.5, 5, 7.5, 10, 12.5, 15, 17.5, or 20 μM
  • Incubation Time: 48 h
  • Method:

    Cells are treated with DMSO control or 2.5, 5, 7.5, 10, 12.5, 15, 17.5, or 20 μM SMAP DT-061 for 48 hours.

Animal Research:

[1]

  • Animal Models: A TKI-resistant EGFR(L858R) patient-derived xenograft (PDX) model (NSG female mice)
  • Dosages: 5 mg/kg
  • Administration: by oral gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 520.52
Formula

C25H23F3N2O5S

CAS No. 1809427-19-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC(C(C(C1)N2C3=CC=CC=C3OC4=CC=CC=C42)O)NS(=O)(=O)C5=CC=C(C=C5)OC(F)(F)F

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01535131 Active not recruiting Procedure: palatoplasty Otitis Media|Cleft Palate University of Pittsburgh|National Institute on Deafness and Other Communication Disorders (NIDCD) February 28 2012 Not Applicable

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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