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MYCi975

Cat. No. M11420
MYCi975 Structure
Synonym:

NUCC-0200975

Size Price Availability Quantity
5mg USD 330  USD330 In stock
10mg USD 530  USD530 In stock
25mg USD 820  USD820 In stock
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Quality Control & Documentation
Biological Activity

MYCi975 (Nuc-0200975) is an orally active MYC inhibitor that disrupts MYC/MAX interactions, promotes MYC T58 phosphorylation and MYC degradation, and impairs myC-driven gene expression. MYCi975 (NUC-0200975) has strong anti-tumor effect and good tolerance, increasing tumor immune cell infiltration and enhancing tumor sensitivity against PD1 immune studies.

Chemical Information
Molecular Weight 561.3
Formula C25H16Cl2F6N2O2
CAS Number 2289691-01-4
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Austin G Holmes, et al. Sci Adv. A MYC inhibitor selectively alters the MYC and MAX cistromes and modulates the epigenomic landscape to regulate target gene expression

[2] Erbao Bian, et al. J Exp Clin Cancer Res. Super-enhancer-associated TMEM44-AS1 aggravated glioma progression by forming a positive feedback loop with Myc

[3] Mihai I Truica, et al. Cancer Res. Turning Up the Heat on MYC: Progress in Small-Molecule Inhibitors

[4] Huiying Han, et al. Cancer Cell. Small-Molecule MYC Inhibitors Suppress Tumor Growth and Enhance Immunotherapy

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  Catalog
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Keywords: MYCi975, NUCC-0200975 supplier, c-Myc, inhibitors, activators


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