Exemestane(FCE 24304)|cas 107868-30-4|DC Chemicals

Cas No.:	107868-30-4
Chemical Name:	Exemestane
Synonyms:	6-Methylene-androsta-1,4-diene-3,17-dione;6-methylenandrosta-1,4-diene-3,17-dione;6-METHYLENEANDROSTA-1,4-DIENE-3,17-DIONE;10,13-dimethyl-6-methylidene-7,8,9,10,11,12,13,14,15,16-decahydrocyclopenta[a]phenanthrene-;EXEMESTANE;FCE-24304;AROMASIN;EXEMESTANCE;ExeMestane(AroMasin);Anti-Estrogen AI Exemestaneknightlabs_leeisun;6-methylenandrost-1,4-diene-3,17-dione;androsta-1,4-diene-6-methylene-3,17-dione;CE24304;EXALAMIDE;EXE;Exemestan;ExemestaneF;FCE 24304;PNU155971;ExeMestine;Exemestane D2;ExeMestane (USP);Exemestanum;Exemestano;Exemestanum [INN-Latin];Exemestano [INN-Spanish];Exemestane [USAN:INN:BAN];FCE24304;Aromasine;NY22HMQ4BX
SMILES:	O=C1C=C2[C@@](C=C1)(C)[C@@H]3[C@@H](CC2=C)[C@H]4[C@@](CC3)(C)C(=O)CC4
Formula:	C₂₀H₂₄O₂
M.Wt:	296.4034
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	Exemestane(FCE 24304) is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.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].
Target:	Aromatase
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.

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