GLPBio

MYCi361

Catalog No.: GC38589Purity:>98.00%Synonyms: NUCC-0196361
MYCi361 is a kind of MYC inhibitor with a KD value for binding to MYC of 3.2μM.

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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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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.

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.

Product Documents

Purity:>98.00%Appearance:A solid

Chemical Properties

CAS No.
2289690-31-7
Synonyms
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
Molecular Formula
C26H16ClF9N2O2
Molecular Weight
594.86
Solubility
DMSO: 110 mg/mL (184.92 mM)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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