DT-061 (SMAP)

Catalog No.S8774 Batch:S877401

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Technical Data

Formula

C25H23F3N2O5S
Molecular Weight 520.52 CAS No. 1809427-19-7
Solubility (25°C)* In vitro DMSO 100 mg/mL (192.11 mM)
Ethanol 50 mg/mL (96.05 mM)
Water 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.)

Preparing Stock Solutions

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]
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 Assay:

[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 Study:

[1]
  • Animal Models

    A TKI-resistant EGFR(L858R) patient-derived xenograft (PDX) model (NSG female mice)

  • Dosages

    5 mg/kg

  • Administration

    by oral gavage

Selleck's DT-061 (SMAP) has been cited by 7 publications

A transcriptional network governing ceramide homeostasis establishes a cytokine-dependent developmental process [ Nat Commun, 2023, 10.1038/s41467-023-42978-w] PubMed: 37945603
Carboxypeptidase A4 negatively regulates HGS-ETR1/2-induced pyroptosis by forming a positive feedback loop with the AKT signalling pathway [ Cell Death Dis, 2023, 14(12):793] PubMed: 38049405
A Wnt-induced lncRNA-DGCR5 splicing switch drives tumor-promoting inflammation in esophageal squamous cell carcinoma [ Cell Rep, 2023, 42(6):112542] PubMed: 37210725
LCK-Mediated RIPK3 Activation Controls Double-Positive Thymocyte Proliferation and Restrains Thymic Lymphoma by Regulating the PP2A-ERK Axis [ Adv Sci (Weinh), 2022, e2204522] PubMed: 36161785
GSK3β is a critical, druggable component of the network regulating the active NOTCH1 protein and cell viability in CLL [ Cell Death Dis, 2022, 13-9:755] PubMed: 36050315
Arid1a regulates cell cycle exit of transit-amplifying cells through inhibiting the Aurka-Cdk1 axis in mouse incisor [ Development, 2021, dev.198838] PubMed: 33766930
Protein Phosphatase 2A Inhibits Gastric Cancer Cell Glycolysis by Reducing MYC Signaling [ Research Square, 2021, 10.21203/rs.3.rs-362391/v1] PubMed: None

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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.

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