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MYCi975 Myc inhibitor

Cat.No.S8906

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. This compound exhibits potent anti-tumor activities.
MYCi975 Myc inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 561.30

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 561.30 Formula

C25H16Cl2F6N2O2

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 2289691-01-4 -- Storage of Stock Solutions

Synonyms NUCC-0200975 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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (178.15 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 60 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.

Mechanism of Action

Targets/IC50/Ki
MYC [1]
In vitro

MYCi975 localizes to the same region of the MYC protei. Treatment of cells with this compound enhances MYC degradation and phosphorylation on T58. It 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]

References

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