SUN-00830
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MedKoo CAT#: 466256

CAS#: unknown

Description: 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).

Chemical Structure

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SUN-00830
CAS# unknown
Instruction

Theoretical Analysis

MedKoo Cat#: 466256
Name: SUN-00830
CAS#: unknown
Chemical Formula: C38H43N11O11
Exact Mass: 829.31
Molecular Weight: 829.828
Elemental Analysis: C, 55.00; H, 5.22; N, 18.57; O, 21.21

Price and Availability

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5mg USD 530 2 Weeks
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Synonym: SUN-00830; SUN00830; SUN 00830; α1A-AR Degrader 9c; α1A AR Degrader 9c; α1AAR Degrader 9c;

IUPAC/Chemical Name: 2-(2-(2-(2-(4-(4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazine-1-carbonyl)-1H-1,2,3-triazol-1-yl)ethoxy)ethoxy)ethoxy)-N-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)acetamide

InChi Key: SFODRSARUJDQSA-UHFFFAOYSA-N

InChi Code: InChI=1S/C38H43N11O11/c1-56-28-18-23-25(19-29(28)57-2)41-38(43-33(23)39)47-10-8-46(9-11-47)36(54)26-20-48(45-44-26)12-13-58-14-15-59-16-17-60-21-31(51)40-24-5-3-4-22-32(24)37(55)49(35(22)53)27-6-7-30(50)42-34(27)52/h3-5,18-20,27H,6-17,21H2,1-2H3,(H,40,51)(H2,39,41,43)(H,42,50,52)

SMILES Code: NC1=NC(N2CCN(CC2)C(C3=CN(N=N3)CCOCCOCCOCC(NC4=CC=CC5=C4C(N(C5=O)C6CCC(NC6=O)=O)=O)=O)=O)=NC7=CC(OC)=C(C=C71)OC

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 83.0 100.00

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Li Z, Lin Y, Song H, Qin X, Yu Z, Zhang Z, Dong G, Li X, Shi X, Du L, Zhao W, Li M. First small-molecule PROTACs for G protein-coupled receptors: inducing α1A-adrenergic receptor degradation. Acta Pharm Sin B. 2020 Sep;10(9):1669-1679. doi: 10.1016/j.apsb.2020.01.014. Epub 2020 Jan 27. PMID: 33088687; PMCID: PMC7563999.