MX69

Catalog No.S8403 Batch:S840301

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Technical Data

Formula

C27H26N2O4S
Molecular Weight 474.57 CAS No. 1005264-47-0
Solubility (25°C)* In vitro DMSO 95 mg/mL (200.18 mM)
Ethanol 41 mg/mL (86.39 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 4.75mg/ml (10.01mM) Taking the 1 mL working solution as an example, add 50 μL of 95 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 clarify; 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.
Clear solution
5% DMSO 95% Corn oil

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 0.675mg/ml (1.42mM) Taking the 1 mL working solution as an example, add 50 μL of 13.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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 MX69 is a MDM2/XIAP inhibitor that binds to MDM2 RING protein with binding Kd values of 2.34 μM. It is used for cancer treatment.
Targets
MDM2 [1]
(Cell-free assay)
2.34 μM(Kd)
In vitro MX69 inhibits expression of both MDM2 and XIAP in a time- and dose-dependent manner. This compound induces ubiquitination of endogenous MDM2 in cancer cells. Downregulation of MDM2 by this chemical is through induction of MDM2 self-ubiquitination and degradation. Half-life of MDM2 in control-treated EU-1 cells is greater than 90 min, whereas this compound treatment decreases the MDM2 half-life to <30 min. In SK-N-SH cells with stably transfected either wild-type (WT)-MDM2 or mutant MDM2-C464A, Treatment with this compound significantly inhibits expression and increased the turnover of WT-MDM2 but not MDM2-C464A. This compound significantly enhances the p53 half-life in WT-MDM2 but not mutant MDM2-C464A-transfected SK-N-SH cells. p53 is stabilized and accumulates in this compound-treated cells. This compound-mediated inhibition of XIAP is MDM2 dependent. Treatment of this chemical activates caspases 3, 7, and 9 as well as the cleavage of the death substrate PARP. This compound also exhibits a significant cytotoxic effect on both ALL and NB lines(cancer cell lines), particularly those lines with MDM2 overexpression and a WTp53 phenotype. This compound-induced cell death is indeed due to apoptosis. This compound-induced cell apoptosis and death are dependent on MDM2, p53, and XIAP expression. This compound shows minimal inhibitory effect on normal human bone marrow in vitro[1].
In vivo MX69 has significant apoptotic and anti-proliferative effects on MDM2-expressing cancer cells in vivo. This compound is well tolerated in animals due to the fact that normal cells/tissues express little or no MDM2. No evidence of toxicity after treatment with this chemical at the 100 mg/kg dose. This MDM2-specific agent should not activate either on-target (e.g., p53 induction) or off-target signaling pathways in normal cells. Thus, specific MDM2 inhibitors such as this compound may be excellent candidates for targeted therapy of refractory cancers expressing high levels of MDM2[1].

Protocol (from reference)

Cell Assay:[1]
  • Cell lines

    six ALL cell lines (EU-1, EU-3, EU-6, EU-8, SUP-B13, and UOC-B1) and six NB cell lines (NB-1691, NB-1643, SH-EP1, IMR-32, SK-NSH, and LA1-55N)

  • Concentrations

    0-10 μM

  • Incubation Time

    24 h

  • Method

    The cytotoxic effect of MX69 is determined using the WST assay. Briefly, cells cultured in 96-well microtiter plates are treated with different concentrations of this compound for a 20-hr period. WST (25 mg/well) is then added and incubation continued for an additional 4 hr, after which the optical density is read with a microplate reader.

References

  • https://pubmed.ncbi.nlm.nih.gov/27666947/

Selleck's MX69 Has Been Cited by 2 Publications

CRLF1 bridges AKT and mTORC2 through SIN1 to inhibit pyroptosis and enhance chemo-resistance in ovarian cancer [ Cell Death Dis, 2024, 15(9):662] PubMed: 39256356
High Glucose Treatment Limits Drosha Protein Expression and Alters AngiomiR Maturation in Microvascular Primary Endothelial Cells via an Mdm2-dependent Mechanism [ Cells, 2021, 10(4)742] PubMed: 33801773

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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.