1375603-36-3

Basic information

• Product Name: VT-464 (raceMate)
• Synonyms: VT-464 (raceMate)
• CAS NO: 1375603-36-3
• Molecular Formula: C18H17F4N3O3
• Molecular Weight: 399.3394928
• Mol File: 1375603-36-3.mol

Chemical Properties

• Boiling Point: 536.3±45.0 °C(Predicted)
• Appearance: /
• Density: 1.393±0.06 g/cm3(Predicted)
• PKA: 8.69±0.70(Predicted)
• CAS DataBase Reference: VT-464 (raceMate)(CAS DataBase Reference)
• NIST Chemistry Reference: VT-464 (raceMate)(1375603-36-3)
• EPA Substance Registry System: VT-464 (raceMate)(1375603-36-3)

Safety Data

• Hazardous Substances Data: 1375603-36-3(Hazardous Substances Data)

Upstream product

• 10103-06-7 2,3-dimethoxynaphthalene 
• 1375603-92-1 C₂₄H₃₁F₄N₃O₄Si 
• 1313885-94-7 C₁₆H₁₄F₄O₃ 
• 404964-94-9 1-(6,7-Dihydroxy-naphthalen-2-yl)-2-methyl-propan-1-one 
• 337522-30-2 1-(6,7-Dimethoxy-naphthalen-2-yl)-2-methyl-propan-1-one 

Downstream Products

• 1610537-15-9 (S)-seviteronel 

Relevant articles and documents

METHODS OF TREATING CANCER USING ANDROGEN RECEPTOR ANTAGONISTS

Disclosed herein are methods of sensitizing cancer cells to an anticancer agent, methods of inhibiting the development of resistance of a cancer cell to an anticancer agent, and methods of inhibiting cancer cell proliferation, each comprising administering an androgen receptor antagonist. Also disclosed herein are methods of determining the prognosis of a subject suffering from cancer, methods of selecting a subject for therapy with an anti-cancer agent and methods of predicting a subject's response to an anti-cancer agent, each comprising determining the level of expression and/or activity of the androgen receptor and/or ZEB1 in the cytoplasm.

COMPOSITIONS FOR THE TREATMENT OF BRAIN TUMORS

The instant invention describes pharmaceutical compositions and dosing regimens comprising radiation therapy and seviteronel with or without dexamethasone, and methods of treating diseases, disorders or symptoms thereof.

COMPOSITIONS FOR THE TREATMENT OF BREAST AND PROSTATE CANCER

The instant invention describes pharmaceutical compositions and dosing regimens comprising seviteronel and/or dexamethasone, and methods of treating diseases, disorders or symptoms thereof.

COMPOSITIONS FOR THE TREATMENT OF BRAIN TUMORS

The instant invention describes pharmaceutical compositions and dosing regimens comprising seviteronel and/or dexamethasone, and methods of treating diseases, disorders symptoms thereof.

Highly-selective 4-(1,2,3-triazole)-based P450c17a 17,20-lyase inhibitors

The orally-active CYP17A1 inhibitor abiraterone acetate (AA) decreases adrenal and intratumoral androgen biosynthesis and is an effective agent for the treatment of prostate cancer. Abiraterone potently inhibits both reactions catalyzed by CYP17, the 17α-hydroxylase (hydroxylase) reaction as well as the 17,20-lyase (lyase) transformation. CYP17 hydroxylase inhibition prevents the synthesis of adrenal glucocorticoids and causes an accumulation of circulating mineralocorticoids. As a consequence of potent CYP17 hydroxylase inhibition (i.e., lack of lyase selectivity), AA must be co-administered with the cortisol replacement prednisone and patients may experience the effects of mineralocorticoid excess syndrome (MES). Herein, we describe rationally-designed, CYP17 lyase-selective inhibitors that could prove safer and more effective than abiraterone. Using proprietary methodology, the high-affinity pyridine or imidazole metal-binding group found in current clinical CYP17 inhibitors was replaced with novel, less avid, metal-binding groups in concert with potency-enhancing molecular scaffold modifications. This process produced a unique series of CYP17 lyase-selective inhibitors that included the oral agent 6 (VT-464), now in Phase 2 prostate cancer clinical trials. The chemical methodology described is potentially applicable to the design of new and more effective metalloenzyme inhibitor treatments for a broad array of diseases.

METALLOENZYME INHIBITOR COMPOUNDS

The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.