CAS 107868-30-4|Exemestane
| Common Name | Exemestane | ||
|---|---|---|---|
| CAS Number | 107868-30-4 | Molecular Weight | 296.403 |
| Density | 1.1±0.1 g/cm3 | Boiling Point | 453.7±45.0 °C at 760 mmHg |
| Molecular Formula | C20H24O2 | Melting Point | 155.13°C |
| MSDS | ChineseUSA | Flash Point | 169.0±25.7 °C |
| Symbol | GHS07, GHS08 | Signal Word | Danger |
Names
| Name | exemestane |
|---|---|
| Synonym | More Synonyms |
Exemestane BiologicalActivity
| Description | Exemestane(FCE 24304) is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.Target: AromataseApproved: October 2005Exemestane competitively inhibits and time-dependently inactivates of human placental aromatase with Ki of 4.3 nM. Exemestane displaces [3H]DHT from rat prostate androgen receptor with IC50 of 0.9 μM [1]. Exemestane (1 μM) increases alkaline phosphatase activity in hFOB and Saos-2 cells and induces the expression of MYBL2, OSTM1, HOXD11, ADCYAP1R1, and glypican 2 in hFOB cells [2]. Exemestane causes aromatase degradation in a dose-responsive manner in MCF-7aro cells [3].Exemestane increases lumbar spine BMD by 14.0% in OVX rats at dose of 100 mg/kg. Exemestane (100 mg/kg) and 17-hydroexemestane (20 mg/kg) significantly reduces an ovariectomy-induced increase in serum pyridinoline and serum osteocalcin in rats and causes significant reductions of serum cholesterol and low-density lipoprotein cholesterol inOVX rats [4].Exemestane (20 mg/kg/day s.c.) induces 26% complete (CR) and 18% partial (PR) tumor regressions in rats with 7,12-dimethylbenzanthracene (DMBA)-induced mammary tumors [5]. |
|---|---|
| Related Catalog | Signaling Pathways >>Others >>AromataseResearch Areas >>Cancer |
| References | [1]. Di Salle, E., et al., Novel aromatase and 5 alpha-reductase inhibitors. J Steroid Biochem Mol Biol, 1994. 49(4-6): p. 289-94. [2]. Miki, Y., et al., Effects of aromatase inhibitors on human osteoblast and osteoblast-like cells: a possible androgenic bone protective effects induced by exemestane. Bone, 2007. 40(4): p. 876-87. [3]. Wang, X. and S. Chen, Aromatase destabilizer: novel action of exemestane, a food and drug administration-approved aromatase inhibitor. Cancer Res, 2006. 66(21): p. 10281-6. [4]. Goss, P.E., et al., Effects of the steroidal aromatase inhibitor exemestane and the nonsteroidal aromatase inhibitor letrozole on bone and lipid metabolism in ovariectomized rats. Clin Cancer Res, 2004. 10(17): p. 5717-23. [5]. Zaccheo, T., D. Giudici, and E. Di Salle, Inhibitory effect of combined treatment with the aromatase inhibitor exemestane and tamoxifen on DMBA-induced mammary tumors in rats. J Steroid Biochem Mol Biol, 1993. 44(4-6): p. 677-80. |
Chemical & Physical Properties
| Density | 1.1±0.1 g/cm3 |
|---|---|
| Boiling Point | 453.7±45.0 °C at 760 mmHg |
| Melting Point | 155.13°C |
| Molecular Formula | C20H24O2 |
| Molecular Weight | 296.403 |
| Flash Point | 169.0±25.7 °C |
| Exact Mass | 296.177643 |
| PSA | 34.14000 |
| LogP | 3.11 |
| Vapour Pressure | 0.0±1.1 mmHg at 25°C |
| Index of Refraction | 1.572 |
| InChIKey | BFYIZQONLCFLEV-DAELLWKTSA-N |
| SMILES | C=C1CC2C(CCC3(C)C(=O)CCC23)C2(C)C=CC(=O)C=C12 |
| Storage condition | Store at -20°C |
Safety Information
| Symbol | GHS07, GHS08 |
|---|---|
| Signal Word | Danger |
| Hazard Statements | H319-H360 |
| Precautionary Statements | P201-P305 + P351 + P338-P308 + P313 |
| Hazard Codes | T,N |
| Risk Phrases | 60-61-51 |
| Safety Phrases | S26-S36/37/39 |
| RIDADR | UN 3261 8/PG 2 |
| WGK Germany | 3 |
| Packaging Group | III |
| Hazard Class | 8 |
| HS Code | 2937900090 |
Customs
| HS Code | 2937900090 |
|---|---|
| Summary | HS: 2937900090 Tax rebate rate:9.0% Supervision conditions:q(report of inspection of soundness on import medicines) VAT:17.0% MFN tariff:4.0% General tariff:30.0% |
Articles67
More Articles| High throughput quantification of prohibited substances in plasma using thin film solid phase microextraction. J. Chromatogr. A. 1374 , 40-9, (2014) Simple, fast and efficient sample preparation approaches that allow high-throughput isolation of various compounds from complex matrices are highly desired in bioanalysis. Particularly sought are meth... | |
| Synergistic effects of combined treatment with simvastatin and exemestane on MCF-7 human breast cancer cells. Mol. Med. Report. 12 , 456-62, (2015) Breast cancer is associated with high levels of incidence, morbidity and mortality; therefore, the identification of effective chemopreventive strategies is crucial. It is important for clinicians to ... | |
| Adjuvant exemestane with ovarian suppression in premenopausal breast cancer. N. Engl. J. Med. 371(2) , 107-18, (2014) Adjuvant therapy with an aromatase inhibitor improves outcomes, as compared with tamoxifen, in postmenopausal women with hormone-receptor-positive breast cancer.In two phase 3 trials, we randomly assi... |
Synonyms
| Exemestan |
| 6-Methylenandrosta-1,4-diene-3,17-dione |
| (8R,9S,10R,13S,14S)-10,13-diméthyl-6-méthylidène-7,8,9,10,11,12,13,14,15,16-décahydro-3H-cyclopenta[a]phénanthrène-3,17(6H)-dione |
| 6-methylenandrost-1,4-diene-3,17-dione |
| Aromasin |
| Exemestane |
| androsta-1,4-diene-6-methylene-3,17-dione |
| (8R,9S,10R,13S,14S)-10,13-dimethyl-6-methylidene-7,8,9,10,11,12,13,14,15,16-decahydro-3H-cyclopenta[a]phenanthrene-3,17(6H)-dione |
| Exemestance |
| 6-Methylene-androsta-1,4-diene-3,17-dione |
| MFCD00866994 |
| 6-Methyleneandrosta-1,4-diene-3,17-dione |
| EXALAMIDE |
| 6-methylideneandrosta-1,4-diene-3,17-dione |
| Androsta-1,4-diene-3,17-dione, 6-methylene- |
| (8R,9S,10R,13S,14S)-10,13-Dimethyl-6-methyliden-7,8,9,10,11,12,13,14,15,16-decahydro-3H-cyclopenta[a]phenanthren-3,17(6H)-dion |
