MYCi361

Catalog No.S8905 Synonyms: NUCC-0196361

For research use only.

MYCi361 is a MYC inhibitor that engages MYC inside cells, disrupts MYC/MAX dimers, and impairs MYC-driven gene expression. MYCi361 binds to MYC with Kd of 3.2 μM. MYCi361 suppresses in vivo tumor growth, increases tumor immune cell infiltration, upregulates PD-L1 on tumors, and sensitizes tumors to anti-PD1 immunotherapy.

MYCi361 Chemical Structure

CAS No. 2289690-31-7

Selleck's MYCi361 has been cited by 1 Publication

Purity & Quality Control

Choose Selective Myc Inhibitors

Biological Activity

Description MYCi361 is a MYC inhibitor that engages MYC inside cells, disrupts MYC/MAX dimers, and impairs MYC-driven gene expression. MYCi361 binds to MYC with Kd of 3.2 μM. MYCi361 suppresses in vivo tumor growth, increases tumor immune cell infiltration, upregulates PD-L1 on tumors, and sensitizes tumors to anti-PD1 immunotherapy.
Targets
MYC [1]
(Cell-free assay)
3.2 μM(Kd)
In vitro

MYCi361 engages MYC inside cells, disrupts MYC/MAX dimers, and impairs MYC-driven gene expression. MYCi361 enhances MYC phosphorylation on threonine-58, consequently increasing proteasome-mediated MYC degradation.[1]

In vivo

MYCi361 suppresses in vivo tumor growth in mice, increases tumor immune cell infiltration, upregulates PD-L1 on tumors, and sensitizes tumors to anti-PD1 immunotherapy.[1]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: MycCaP, PC3, LNCaP, PC12, MV411, SK-N-BE (2), 293T, P493-6 B cells, LLC1, TGR-1, HO15.19 Rat-1 cells
  • Concentrations: 4 μM
  • Incubation Time: 72 h
  • Method:

    Immunogenic Cell Death Assays: MycCaP cells are treated with 4 μM MYCi361 for 72 hr, and supernatants are collected. Cell counts are performed for quantifying secreted ATP and high mobility group protein B1 (HMGB1). For detection of surface Calreticulin, cells are incubated with rabbit anti-Calreticulin for 60 min and then incubated with Alexa Flour 488 anti-rabbit secondary antibody, and analyzed by flow cytometry.

Animal Research:

[1]

  • Animal Models: 6-8 week old FVB mice, prostate PDX model, NSG mice, C57BL/6 mice, CB17/Icr-Prkdcscid/IcrIcoCrl mice, CD-1 mice
  • Dosages: 55 mg/kg, 50 mg/kg
  • Administration: IP, Oral gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 594.86
Formula

C26H16ClF9N2O2

CAS No. 2289690-31-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1C(=CC(=N1)C(F)(F)F)C2=C(C(=C(C=C2)OCC3=CC=C(C=C3)Cl)C4=CC(=CC(=C4)C(F)(F)F)C(F)(F)F)O

In vivo Formulation Calculator (Clear solution)

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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.

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Molarity Calculator

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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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