PeptideDB

SDU-071

SDU-071

CAS No.:

SDU-071 is a potent and orally active BRD4-p53 inhibitor. SDU-071 inhibits the proliferation of MDA-MB-231 cells with an
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SDU-071 is a potent and orally active BRD4-p53 inhibitor. SDU-071 inhibits the proliferation of MDA-MB-231 cells with an IC50 of 10.5 μM. SDU-071 induces cell cycle arrest and apoptosis.

Physicochemical Properties


Molecular Formula C28H25N3O2
Molecular Weight 435.52
Appearance Light yellow to yellow solid powder
HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage.(2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture.
Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


ln Vitro SDU-071 (10 μM, 24 h) induces cell cycle arrest and apoptosis in MDA-MB-231 cells[1]. SDU-071 (10 μM, 72 h) inhibits the proliferation, migration and invasion of MDA-MB-231 cells[1].
ln Vivo SDU-071 (250 mg/kg, gavage; once daily for 21 days) inhibits tumor growth in the MDA-MB-231 orthotopic mouse breast xenograft tumor model [1].
Cell Assay Apoptosis Analysis[1]
Cell Types: MDA-MB-231cells Tested
Tested Concentrations: 2.5, 5, and 10 μM
Incubation Duration: 24 hours
Experimental Results: Altered cell cycle progression in the G1, S, and G2/M phases. Induced apoptosis in MDA-MB-231 cells.
Animal Protocol Animal/Disease Models: DA-MB-231 Orthotopic Mouse Xenograft Mammary Tumor Model[1]
Doses: 50 and 250 mg/kg; Once daily for 21 days
Route of Administration: Gavage administration (i.g.)
Experimental Results: Significantly inhibited tumor growth with 49.1% inhibition. Reduced the Protein levels for BRD4, Mucin5AC, c-Myc, CDK4, and CDK6, upregulated the p21 protein.
References

[1]. Novel BRD4-p53 Inhibitor SDU-071 Suppresses Proliferation and Migration of MDA-MB-231 Triple-Negative Breast Cancer CellsJ. ACS Pharmacology & Translational Science, 2024.


Solubility Data


Solubility (In Vitro) DMSO : ~100 mg/mL (~229.61 mM; with ultrasonication)
Solubility (In Vivo) Solubility in Formulation 1: ≥ 4 mg/mL (9.18 mM)(saturation unknown) in 10% DMSO 40% PEG300 5% Tween-80 45% Saline (add these co-solvents sequentially from left to right, and one by one),clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 40.0 mg/mL clear DMSO stock solution and add it to 400 μL PEG300, mix well; then add 50 μL Tween-80 to the above system, mix well; then continue to add 450 μL of normal saline to make up to 1 mL. Preparation of normal saline: Dissolve 0.9 g of sodium chloride in ddH₂O and make up to 100 mL to obtain a clear and transparent normal saline solution.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.2961 mL 11.4805 mL 22.9611 mL
5 mM 0.4592 mL 2.2961 mL 4.5922 mL
10 mM 0.2296 mL 1.1481 mL 2.2961 mL
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.