Home Cell Cycle Myc inhibitor MYCi975 For research use only.

MYCi975

Synonyms: NUCC-0200975

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.

MYCi975 Chemical Structure

MYCi975 Chemical Structure

CAS No. 2289691-01-4

Purity & Quality Control

MYCi975 Related Products

Signaling Pathway

Myc Signaling Pathways

Myc Signaling Pathway

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
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]
Cell Research 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.
In Vivo
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]
Animal Research 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

Chemical Information & Solubility

Molecular Weight 561.30 Formula

C25H16Cl2F6N2O2
CAS No. 2289691-01-4 SDF --
Smiles CN1C(=CC(=N1)C(F)(F)F)C2=C(C(=C(C=C2)OCC3=CC=C(C=C3)Cl)C4=CC(=C(C=C4)Cl)C(F)(F)F)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (178.15 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 60 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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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.
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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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