GLPBio

MYCi361

Catalog No.: GC38589Purity:>98.00%Synonyms: NUCC-0196361
COASDSData Sheet
MYCi361 (NUCC-0196361) est un inhibiteur de MYC avec un Kd de 3,2 μM pour la liaison À MYC. MYCi361 (NUCC-0196361) supprime la croissance tumorale et améliore l'immunothérapie anti-PD1.

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MYCi361
Cas No.: 2289690-31-7
10mM (in 1mL DMSO)In Stock
$204.00
1
1mgIn Stock
$71.00
1
5mgIn Stock
$156.00
1
10mgIn Stock
$231.00
1
25mgIn Stock
$357.00
1
50mgIn Stock
$527.00
1
100mgIn Stock
$709.00
1
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Citations

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    Nature
    641, 529–536 (2025)
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    632, 686–694 (2024)
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    618, 1017–1023 (2023)
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    Nature
    610, 366–372 (2022)
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    Cell
    187(9):2288-2304 (2024)
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    Cell
    183(7):1867-1883 (2020)
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    Science
    388(6745) (2025)
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    387(6734) (2025)
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    35, 97–116 (2025)
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    34, 683–706 (2024)
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    33, 273–287 (2023)
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    33, 904–922 (2023)
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    31, 1291–1307 (2021)

Description

MYCi361 is a kind of MYC inhibitor with a KD value for binding to MYC of 3.2μM [1]. MYCi361 can bind to MYC and disrupt MYC/MAX complex formation, while also decrease MYC protein stability, which lead to significant inhibition of MYC-dependent cancer-cell proliferation in vitro and inhibition of tumor growth in vivo [1]. MYCi361 showed excellent pharmacokinetic profiles, with long terminal half-lives, high peak plasma concentration, and tumor penetration [1].

MYCi361 (0~20μM; 5d) inhibited the viability of MYC-dependent cancer cells including prostate cancer (Myc-CaP, LNCaP, and PC3), leukemia (MV4-11), lymphoma (HL-60 and P493-6), and neuroblastoma (SK-N-B2) [1]. MYCi361 (6μM; 24h) inhibited the cell proliferation of primary prostate cancer cells [2].

MYCi361 (50mg/kg; bid; 2d; i.p.) induced tumor regression in FVB mice bearing established MycCaP tumor [1]. MYCi361 (55mg/kg; 42d; i.p.) significant decreased the tumor’s size and weight in NOD/SCID/IL2rg-/-(NSG) mice transplanted prostate cancer tumor tissues [2].

References:
[1] Han H, Jain A D, Truica M I, et al. Small-molecule MYC inhibitors suppress tumor growth and enhance immunotherapy [J]. Cancer Cell, 2019, 36(5): 483-97.e15.
[2] Ding T, Zhu Y, Jin H, et al. Circular RNA circ_0057558 controls prostate cancer cell proliferation through regulating miR-206/USP33/c-Myc axis [J]. Frontiers in cell and developmental biology, 2021, 9: 644397.

Protocole (Protocol)

Cell experiment [1]:

Cell lines

Primary prostate cancer cells

Preparation Method

The cells were plated onto 96-well plates, cultured overnight, and then treated with 6µM MYCi361 or vehicle (DMSO). After 48h of culture, CCK-8 reagent was added and incubated at 37℃, 5% CO2 for another 1h. The optical density was recorded at 450nm (OD450) using a microplate reader. The inhibition rate of cell proliferation was calculated.

Reaction Conditions

6μM; 24h

Applications

MYCi361 inhibited the cell proliferation of primary prostate cancer cells.

Animal experiment [2]:

Animal models

Male FVB mice

Preparation Method

MycCaP Ebox-Luc cells suspended in 100ml BD matrigel were subcutaneously injected into flanks of mice to establish MycCaP allograft prostate mouse model. MYCi361 was dissolved in PBS with 10% DMSO and 20% Tween 80. Then the mice were treated with MYCi361 initially at 50mg/kg twice daily for 2 days. Caliper measurement of tumor size were performed after treatment.

Dosage form

50mg/kg; bid; 2d; i.p.

Applications

MYCi361 induced tumor regression in FVB mice bearing established MycCaP tumor.

References:
[1] Ding T, Zhu Y, Jin H, et al. Circular RNA circ_0057558 controls prostate cancer cell proliferation through regulating miR-206/USP33/c-Myc axis [J]. Frontiers in cell and developmental biology, 2021, 9: 644397.
[2] Han H, Jain A D, Truica M I, et al. Small-molecule MYC inhibitors suppress tumor growth and enhance immunotherapy [J]. Cancer Cell, 2019, 36(5): 483-97.e15.

Documents produit (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Propriétés chimiques (Chemical Properties)

N° CAS
2289690-31-7
Synonymes
NUCC-0196361
SMILES
ClC1=CC=C(COC2=CC=C(C3=CC(C(F)(F)F)=NN3C)C(O)=C2C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)C=C1
Formule moléculaire
C26H16ClF9N2O2
Masse moléculaire
594.86
Solubilité
DMSO: 110 mg/mL (184.92 mM)
Conservation
Store at -20°C
Conseils généraux
Choisissez un solvant adapté selon les données de solubilité du produit. Après préparation, répartissez la solution mère en aliquotes afin d’éviter les cycles répétés de congélation-décongélation.
Utilisez les solutions mères dans les 6 mois si elles sont conservées à -80°C, ou dans le mois si elles sont conservées à -20°C.
Pour améliorer la solubilité, réchauffez le tube à 37°C et soniquez-le pendant une durée appropriée.
Conditions d’expédition
Les échantillons d’évaluation sont expédiés avec des blocs réfrigérants. Les autres formats sont expédiés à température ambiante ou, sur demande, avec des blocs réfrigérants.

Calculateurs (Calculators)Molarité / Dilution / Masse moléculaire / Conversion d’unités / Formulation in vivo / Solubilité

g/mol

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