264130-01-0

Basic information

• Product Name: 11β-[4-(N,N-dimethylamino)-phenyl]-17α-(3-methyl-1-butynyl)-estra-9-en-5α,17β-diol-3-one, cyclic 1,2-ethandiyl acetal
• Synonyms: 11β-[4-(N,N-dimethylamino)-phenyl]-17α-(3-methyl-1-butynyl)-estra-9-en-5α,17β-diol-3-one, cyclic 1,2-ethandiyl acetal
• CAS NO: 264130-01-0
• Molecular Weight: 519.725
• Mol File: 264130-01-0.mol
• Article Data: 2

Chemical Properties

• CAS DataBase Reference: 11β-[4-(N,N-dimethylamino)-phenyl]-17α-(3-methyl-1-butynyl)-estra-9-en-5α,17β-diol-3-one, cyclic 1,2-ethandiyl acetal(CAS DataBase Reference)
• NIST Chemistry Reference: 11β-[4-(N,N-dimethylamino)-phenyl]-17α-(3-methyl-1-butynyl)-estra-9-en-5α,17β-diol-3-one, cyclic 1,2-ethandiyl acetal(264130-01-0)
• EPA Substance Registry System: 11β-[4-(N,N-dimethylamino)-phenyl]-17α-(3-methyl-1-butynyl)-estra-9-en-5α,17β-diol-3-one, cyclic 1,2-ethandiyl acetal(264130-01-0)

Safety Data

• Hazardous Substances Data: 264130-01-0(Hazardous Substances Data)

Upstream product

• 598-23-2 3-methyl-but-1-yne 
• 264130-00-9 estra-5α,10α-epoxy-9(11)-en-3-one, 17β-hydroxy-17α-(3-methyl-1-butynyl) cyclic 3-(1,2-ethanediyl acetal) 
• 7353-91-5 4-dimethylaminophenylmagnesium bromide 
• 264129-99-9 estra-5(10),9(11)-dien-3-one, 17β-hydroxy-17α-(3-methyl-1-butynyl) cyclic 3-(1,2-ethanediyl acetal) 
• 5571-36-8 ethylene deltenone 
• 586-77-6 4-bromo-N,N-dimethylaniline 

Relevant articles and documents

Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101)

The glucocorticoid receptor (GR) has been linked to therapy resistance across a wide range of cancer types. Preclinical data suggest that antagonists of this nuclear receptor may enhance the activity of anticancer therapy. The first-generation GR antagonist mifepristone is currently undergoing clinical evaluation in various oncology settings. Structure-based modification of mifepristone led to the discovery of ORIC-101 (28), a highly potent steroidal GR antagonist with reduced androgen receptor (AR) agonistic activity amenable for dosing in androgen receptor positive tumors and with improved CYP2C8 and CYP2C9 inhibition profile to minimize drug-drug interaction potential. Unlike mifepristone, 28 could be codosed with chemotherapeutic agents readily metabolized by CYP2C8 such as paclitaxel. Furthermore, 28 demonstrated in vivo antitumor activity by enhancing response to chemotherapy in the GR+ OVCAR5 ovarian cancer xenograft model. Clinical evaluation of safety and therapeutic potential of 28 is underway.