MYCi361

Catalog No.S8905 Batch:S890501

Technical Data

Formula

C₂₆H₁₆ClF₉N₂O₂

Molecular Weight

594.86

CAS No.

2289690-31-7

Solubility (25°C)*

In vitro

DMSO

100 mg/mL (168.1 mM)

Ethanol

14 mg/mL (23.53 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution

5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O

2.5mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

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.

Targets

MYC ^[1]
(Cell-free assay)

3.2 μM(Kd)

In vitro

MYCi361 engages MYC inside cells, disrupts MYC/MAX dimers, and impairs MYC-driven gene expression. MYCi361 enhances MYC phosphorylation on threonine-58, consequently increasing proteasome-mediated MYC degradation.^[1]

In vivo

MYCi361 suppresses in vivo tumor growth in mice, increases tumor immune cell infiltration, upregulates PD-L1 on tumors, and sensitizes tumors to anti-PD1 immunotherapy.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines MycCaP, PC3, LNCaP, PC12, MV411, SK-N-BE (2), 293T, P493-6 B cells, LLC1, TGR-1, HO15.19 Rat-1 cells Concentrations 4 μM Incubation Time 72 h Method Immunogenic Cell Death Assays: MycCaP cells are treated with 4 μM MYCi361 for 72 hr, and supernatants are collected. Cell counts are performed for quantifying secreted ATP and high mobility group protein B1 (HMGB1). For detection of surface Calreticulin, cells are incubated with rabbit anti-Calreticulin for 60 min and then incubated with Alexa Flour 488 anti-rabbit secondary antibody, and analyzed by flow cytometry.
Animal Study:^{^[1]}	Animal Models 6-8 week old FVB mice, prostate PDX model, NSG mice, C57BL/6 mice, CB17/Icr-Prkdcscid/IcrIcoCrl mice, CD-1 mice Dosages 55 mg/kg, 50 mg/kg Administration IP, Oral gavage

Cell Assay:^{^[1]}

Cell lines
MycCaP, PC3, LNCaP, PC12, MV411, SK-N-BE (2), 293T, P493-6 B cells, LLC1, TGR-1, HO15.19 Rat-1 cells
Concentrations
4 μM
Incubation Time
72 h
Method
Immunogenic Cell Death Assays: MycCaP cells are treated with 4 μM MYCi361 for 72 hr, and supernatants are collected. Cell counts are performed for quantifying secreted ATP and high mobility group protein B1 (HMGB1). For detection of surface Calreticulin, cells are incubated with rabbit anti-Calreticulin for 60 min and then incubated with Alexa Flour 488 anti-rabbit secondary antibody, and analyzed by flow cytometry.

Animal Study:^{^[1]}

Animal Models
6-8 week old FVB mice, prostate PDX model, NSG mice, C57BL/6 mice, CB17/Icr-Prkdcscid/IcrIcoCrl mice, CD-1 mice
Dosages
55 mg/kg, 50 mg/kg
Administration
IP, Oral gavage

References

[1] Huiying Han, et al. Cancer Cell. 2019 Nov 11;36(5):483-497.e15.

Selleck's MYCi361 has been cited by 4 publications

Inhibiting BRAF/EGFR/MEK suppresses cancer stemness and drug resistance of primary colorectal cancer cells [ Oncotarget, 2023, 14:879-889]	PubMed: 37791907
Inhibiting BRAF/EGFR/MEK suppresses cancer stemness and drug resistance of primary colorectal cancer cells [ Oncotarget, 2023, 10.18632/oncotarget.28517]	PubMed: 37791907
Loss of G0/G1 switch gene 2 (G0S2) promotes disease progression and drug resistance in chronic myeloid leukaemia (CML) by disrupting glycerophospholipid metabolism [ Clin Transl Med, 2022, 12(12):e1146]	PubMed: 36536477
Circular RNA circ_0057558 Controls Prostate Cancer Cell Proliferation Through Regulating miR-206/USP33/c-Myc Axis [ Front Cell Dev Biol, 2021, 9:644397]	PubMed: 33718387

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.