SUN-00830 is a selective α1A-adrenergic receptor Degrader (PROTAC®; DC50 = 2.86 µM, 94% α1A-adrenoceptor degradation at 10 µM for 12 h). It comprises the α-adrenoceptor antagonist Prazosin, joined by a linker to a cereblon ligand Pomalidomide. SUN-00830 selectively downregulates α1A-adrenoceptor levels, but not α1B-AR and α1D-AR in HEK293 cells. SUN-00830 shows concentration-dependent antiproliferative activity in PC-3 prostate cancer cells (IC50 = 6.12 µM) in vitro, and PC-3 tumor xenografts in vivo. This product has no formal name. For the convenience of scientific communication, we named it by combining its InChi Key (3 letters from the first letter of each section) with the last 5 digit of its CAS#) according to MedKoo Chemical Nomenclature (https://www.medkoo.com/page/naming).
MedKoo Cat#: 466256
Name: SUN-00830
CAS#: unknown
Chemical Formula: C38H43N11O11
Exact Mass: 829.3144
Molecular Weight: 829.83
Elemental Analysis: C, 55.00; H, 5.22; N, 18.57; O, 21.21
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 83.0 | 100.00 |
The following data is based on the product molecular weight 829.83 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
