PROTAC BRD4 Degrader-11 (compound 9a) is a potent PROTAC linked to a von Hippel-Lindau ligand and a BRD4 ligand. PROTAC BRD4 Degrader-11 can conjugate with STEAP1 and CLL1 antibodies to degrade BRD4 protein in PC3 prostate cancer cells with DC50s of 0.23 nM and 0.38 nM respectively.

Physicochemical Properties

Molecular Formula	C61H75F2N9O12S4
Molecular Weight	1292.56
Appearance	Off-white to light 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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light.
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

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 :~100 mg/mL (~77.37 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (1.93 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 25.0 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	0.7737 mL	3.8683 mL	7.7366 mL
	5 mM	0.1547 mL	0.7737 mL	1.5473 mL
	10 mM	0.0774 mL	0.3868 mL	0.7737 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.