159354-61-7

Basic information

• Product Name: 1α,2α-epoxy-6-methylenandrost-4-ene-3,17-dione
• CAS NO: 159354-61-7
• Molecular Weight: 312.409
• Mol File: 159354-61-7.mol
• Article Data: 2

Chemical Properties

• Boiling Point: 480.1±45.0 °C(Predicted)
• Density: 1.22±0.1 g/cm3(Predicted)
• CAS DataBase Reference: 1α,2α-epoxy-6-methylenandrost-4-ene-3,17-dione(CAS DataBase Reference)
• NIST Chemistry Reference: 1α,2α-epoxy-6-methylenandrost-4-ene-3,17-dione(159354-61-7)
• EPA Substance Registry System: 1α,2α-epoxy-6-methylenandrost-4-ene-3,17-dione(159354-61-7)

Safety Data

• Hazardous Substances Data: 159354-61-7(Hazardous Substances Data)

Usage

Uses

1,2-α-Epoxy Exemestane is a metabolite of Exemestane (E957000); a third-generation steroidal aromatase inhibitor that has been used in clinics for hormone-dependent breast cancer treatment in post-menopausal women.

Upstream product

• 107868-30-4 exemestane 

Relevant articles and documents

Oxymestane, a cytostatic steroid derivative of exemestane with greater antitumor activity in non-estrogen-dependent cell lines

A new promising steroid derivative of Exemestane (Exe), the drug used for the treatment of estrogen-dependent breast cancer, was synthesized and evaluated against a set of human cancer cell lines. The new compound (Oxymestane-D1, Oxy) was tested comparatively with Exe against colon (C2BBe1, WiDr), liver (HepG2, HuH-7), lung (A549, H1299) and prostate (LNCaP, PC3) human cancer cell lines. Likewise, its effect on human colon normal cells (CCD-841 CoN) and human normal fibroblast cells (HFF-1) was studied. The cytostatic activity of Oxy was also compared with that of the reference cytostatic drugs used in chemotherapy protocols, namely carboplatin, cisplatin, doxorubicin, epirubicin, etoposide, flutamide, 5-fluorouracil, irinotecan, oxaliplatin and sorafenib. In all cell lines tested, Oxy proved to be more powerful cytostatic than Exe. Additionally, the IC50 at 72 h showed a three-fold activity greater than 5-fluorouracil in the WiDr cell line, twice as high as cisplatin for cell line A549 and five times higher than cisplatin for cell line H1299. Also, Oxy surprisingly revealed to induce DNA damage and inhibit the DNA damage response (DDR) proteins ATM, ATR, CHK1 and CHK2. The results obtained allow concluding that Oxy can be a promising anticancer agent to be used in chemotherapy protocols. Furthermore, its ability to inhibit crucial components of DDR can also be useful for the monotherapy or for combination with chemo and/or radiotherapy of cancer.