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107868-30-4

107868-30-4 structure
107868-30-4 structure
  • Name: Exemestane
  • Chemical Name: exemestane
  • CAS Number: 107868-30-4
  • Molecular Formula: C20H24O2
  • Molecular Weight: 296.403
  • Catalog: API Antineoplastic agents Hormone antineoplastic agents
  • Create Date: 2018-02-24 08:00:00
  • Modify Date: 2024-01-02 19:07:18
  • 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].
Name exemestane
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
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
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.
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
Storage condition Store at -20°C
Symbol GHS07 GHS08
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
19457-55-7 structure

19457-55-7

~82%

107868-30-4 structure

107868-30-4
Literature: Crystal Pharma, S.A. Patent: EP2070943 A1, 2009 ; Location in patent: Page/Page column 9 ;
933455-74-4 structure

933455-74-4

~88%

107868-30-4 structure

107868-30-4
Literature: Pariza, Richard J.; Yarger, James G. Patent: US2007/88013 A1, 2007 ; Location in patent: Page/Page column 3 ;
861395-77-9 structure

861395-77-9

~%

107868-30-4 structure

107868-30-4
Literature: WO2005/70951 A1, ; Page/Page column 18-24 ;
122370-91-6 structure

122370-91-6

~99%

107868-30-4 structure

107868-30-4
Literature: Marcos-Escribano, Andres; Bermejo, Francisco A.; Bonde-Larsen, Antonio Lorente; Retuerto, Jesus Iglesias; Sierra, Ignacio Herraiz Tetrahedron, 2009 , vol. 65, # 36 p. 7587 - 7590
7440-44-0 structure

7440-44-0
19457-55-7 structure

19457-55-7
75-65-0 structure

75-65-0

~%

107868-30-4 structure

107868-30-4
Literature: US4808616 A1, ;
846-48-0 structure

846-48-0

~%

107868-30-4 structure

107868-30-4
Literature: Steroids, , vol. 58, # 11 p. 527 - 532
897-06-3 structure

897-06-3

~%

107868-30-4 structure

107868-30-4
Literature: Pharmazie, , vol. 61, # 7 p. 575 - 581
67737-88-6 structure

67737-88-6

~%

107868-30-4 structure

107868-30-4
Literature: Pharmazie, , vol. 61, # 7 p. 575 - 581
53-43-0 structure

53-43-0

~%

107868-30-4 structure

107868-30-4
Literature: Steroids, , vol. 78, # 11 p. 1148 - 1151
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%

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