別品名 |
Certican
|
別包装 |
あり
|
純度 |
>=98%
|
分子量 |
958.22
|
CAS RN® |
159351-69-6
|
化合物の概要 |
mTORC1 inhibitor.
|
構造 |
C53H83NO14
|
溶媒 |
Insoluble in water. Soluble in DMSO (30mg/mL), ethanol (7 mg/mL).
|
使用目的 |
Everolimus is an inhibitor of mammalian target of rapamycin 1 (mTOR1) that is used clinically for its immunosuppressive activity in renal transplant recipients and is currently in clinical trials exploring its anticancer chemotherapeutic activity. In nasopharyngeal carcinoma cells, everolimus induces apoptosis and autophagy, inhibiting cell growth. In esophageal cancer cells, everolimus decreases expression of mTOR targets p70S6K and S6, increasing cell damage and decreasing cell proliferation. In animal models of experimental autoimmune uveoretinitis (EAU), everolimus decreases levels of Th1, Th2, and Th17 cytokines and increases levels of Treg cells, attenuating disease pathology. Additionally, everolimus exhibits nephroprotective benefit at low doses, decreasing adriamycin-induced proteinuria and improving renal function in animal models of nephrotic syndrome.
|
その他 |
[融点]95-110℃
|
参考文献 |
Sendur MA, Zengin N, Aksoy S, et al. Everolimus: a new hope for patients with breast cancer. Curr Med Res Opin. 2014 Jan;30(1):75-87. PMID: 24050600.Cai Y, Xia Q, Su Q, et al. mTOR inhibitor RAD001 (everolimus) induces apoptotic, not autophagic cell death, in human nasopharyngeal carcinoma cells. Int J Mol Med. 2013 Apr;31(4):904-12. PMID: 23426850.Hennig M, Bauer D, Wasmuth S, et al. Everolimus improves experimental autoimmune uveoretinitis. Exp Eye Res. 2012 Dec;105:43-52. PMID: 23059401.Ramadan R, Faour D, Awad H, et al. Early treatment with everolimus exerts nephroprotective effect in rats with adriamycin-induced nephrotic syndrome. Nephrol Dial Transplant. 2012 Jun;27(6):2231-41. PMID: 22036940.Wang ZG, Fukazawa T, Nishikawa T, et al. RAD001 offers a therapeutic intervention through inhibition of mTOR as a potential strategy for esophageal cancer. Oncol Rep. 2010 Apr;23(4):1167-72. PMID: 20204306.Kahan BD, Koch SM. Current immunosuppressant regimens: considerations for critical care. Curr Opin Crit Care. 2001 Aug;7(4):242-50. PMID: 11571421.
|
※サムネイル画像をクリックすると拡大画像が表示されます。
|
|
|
メーカー |
品番 |
包装 |
LKT
|
E8419
|
5 MG
|
※表示価格について
当社在庫 |
なし
|
納期目安 |
1週間程度
|
保存温度 |
常温
|
|