PROTAC BRD4 Degrader-8 is a PROTAC linked to a von Hippel-Lindau ligand and a BRD4 ligand with IC50s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 can effectively degrade BRD4 protein in PC3 prostate cancer cells.

Physicochemical Properties

Molecular Formula	C53H61F2N9O11S2
Molecular Weight	1102.23
Appearance	White to off-white 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: This product requires protection from light (avoid light exposure) during transportation and storage.
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

Targets	IC50: 1.1 nM (BRD4 BD1), 1.4 nM (BRD4 BD2)[1]
ln Vitro	At an IC50 of 28 nM, PROTAC BRD4 Degrader-8 (Compound 8; 6 days) stops PC3 prostate cancer cells from proliferating [1]. MYC gene transcription in MV4-11 AML cells is inhibited by PROTAC BRD4 Degrader-8(4 h) with an IC50 of 11 nM[1]. At a DC50 of 7.5 nM, PROTAC BRD4 Degrader-8(4 h) efficiently breaks down BRD4 protein in PC3 prostate cancer cells[1].
References	[1]. Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy. J Med Chem. 2021 Mar 11;64(5):2576-2607.

Solubility Data

Solubility (In Vitro)

DMSO :~90 mg/mL (~81.65 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 4.5 mg/mL (4.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 45.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 4.5 mg/mL (4.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 45.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	0.9073 mL	4.5363 mL	9.0725 mL
	5 mM	0.1815 mL	0.9073 mL	1.8145 mL
	10 mM	0.0907 mL	0.4536 mL	0.9073 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.