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MYCi361

Cat. No. M20729
MYCi361 Structure
Synonym:

NUCC-0196361

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Biological Activity

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.

Chemical Information
Molecular Weight 594.86
Formula C26H16ClF9N2O2
CAS Number 2289690-31-7
Solubility (25°C) DMSO 100 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] Sofia Gialesaki, et al. Blood. RUNX1 isoform disequilibrium promotes the development of trisomy 21 associated myeloid leukemia

[2] Tao Ding, et al. Front Cell Dev Biol. Circular RNA circ_0057558 Controls Prostate Cancer Cell Proliferation Through Regulating miR-206/USP33/c-Myc Axis

[3] 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: MYCi361, NUCC-0196361 supplier, c-Myc, inhibitors, activators


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