PROTAC AR/AR-V7 degrader-1 (27c) is a dual PROTAC degrader for AR and AR-V7 with DC50 values of 2.67 and 2.64 μM, respectively. PROTAC AR/AR-V7 degrader-1 (27c) can induce apoptosis (Red: AR antagonist; Blue: E3 ligase ligand; Black: linker).

Physicochemical Properties

Molecular Formula	C24H19F4N5O2
Molecular Weight	485.43
CAS #	2841308-96-9
Appearance	Off-white to yellow solid powder
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

ln Vitro	PROTAC AR/AR-V7 degrader-1 (27c) effectively inhibits the transcriptional activity of the AR signaling pathway. In 22RV1 cells, the IC50 of PROTAC AR/AR-V7 degrader-1 (27c) is 0.9 μM[1]. PROTAC AR/AR-V7 degrader-1 (27c) overcomes drug resistance in advanced prostate cancer expressing AR splice variants[1].
References	[1]. Structure–Activity Relationship (SAR) Studies of Novel Monovalent AR/AR-V7 Dual Degraders with Potent Efficacy against Advanced Prostate Cancer. J. Med. Chem. 2024, 67, 7, 5567-5590.

Solubility Data

Solubility (In Vitro)

DMSO : ≥ 100 mg/mL (~206.00 mM)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.0600 mL	10.3001 mL	20.6003 mL
	5 mM	0.4120 mL	2.0600 mL	4.1201 mL
	10 mM	0.2060 mL	1.0300 mL	2.0600 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.