MYCi975

Catalog No.S8906 Batch:S890602

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Technical Data

Formula

C25H16Cl2F6N2O2
Molecular Weight 561.30 CAS No. 2289691-01-4
Solubility (25°C)* In vitro DMSO 100 mg/mL (178.15 mM)
Ethanol 100 mg/mL (178.15 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.)

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Biological Activity

Description MYCi975 (NUCC-0200975) is a potent, selective and orally active inhibitor of MYC that disrupts MYC/MAX interaction, promotes MYC T58 phosphorylation and MYC degradation, and impairs MYC driven gene expression. MYCi975 exhibits potent anti-tumor activities.
Targets
MYC [1]

Biological Activity

Description MYCi975 (NUCC-0200975) is a potent, selective and orally active inhibitor of MYC that disrupts MYC/MAX interaction, promotes MYC T58 phosphorylation and MYC degradation, and impairs MYC driven gene expression. MYCi975 exhibits potent anti-tumor activities.
Targets
MYC [1]
In vitro

MYCi975 localizes to the same region of the MYC protei. Treatment of cells with MYCi975 enhances MYC degradation and phosphorylation on T58. MYCi975 also directly increases GSK3b-mediated MYC pT58 in the in vitro kinase assay.[1]
In vivo

MYCi975 suppresses in vivo tumor growth in mice, increases tumor immune cell infiltration, upregulates PD-L1 on tumors, and sensitizes tumors to anti-PD1 immunotherapy with good tolerability.[1]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    MycCaP, PC3, LNCaP, PC12, MV411, SK-N-BE (2), 293T, P493-6 B cells, LLC1 cells, TGR-1, HO15.19 Rat-1 cells

  • Concentrations

    3-25 μM, 8 μM, 6 μM

  • Incubation Time

    24 h

  • Method

    PC3 cells are treated with 6 μM 361 or 8 μM 975 and P493-6 cells are treated with 0.1 mg/ml Tetracycline or 6 μM 975 for 24 hr in triplicates. Then cells are washed with PBS and RNA is extracted using RNAeasy Plus mini kit.
Animal Study:

[1]
  • Animal Models

    6-8 weeks old FVB mice, prostate PDX model (TM00298), NSG mice, C57BL/6, CB17/Icr-Prkdcscid/IcrIcoCrl mice, CD-1

  • Dosages

    50 mg/kg, 100 mg/kg

  • Administration

    IP

Selleck's MYCi975 has been cited by 7 publications

The oncogenic axis YAP/MYC/EZH2 impairs PTEN tumor suppression activity enhancing lung tumorigenicity [ Cell Death Discov, 2024, 10(1):452] PubMed: 39455556
A program of successive gene expression in mouse one-cell embryos [ Cell Rep, 2023, 42(2):112023] PubMed: 36729835
Patient-Derived Triple-Negative Breast Cancer Organoids Provide Robust Model Systems That Recapitulate Tumor Intrinsic Characteristics [ Cancer Res, 2022, 82(7):1174-1192] PubMed: 35180770
Loss of G0/G1 switch gene 2 (G0S2) promotes disease progression and drug resistance in chronic myeloid leukaemia (CML) by disrupting glycerophospholipid metabolism [ Clin Transl Med, 2022, 12(12):e1146] PubMed: 36536477
MEK/ERK-mediated oncogenic signals promote secretion of extracellular vesicles by controlling lysosome function [ Cancer Sci, 2022, 113(4):1264-1276] PubMed: 35108425
Yap-Myc signaling induces pancreatic stellate cell activation through regulating glutaminolysis [ Exp Cell Res, 2022, 411(1):113000] PubMed: 34958764
Patient-derived triple negative breast cancer organoids provide robust model systems that recapitulate tumor intrinsic characteristics [ bioRxiv, 2021, 10.1101/2021.08.09.455691] 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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.