Bioactivity | LY117018 TFA, a Raloxifene analog, is a selective estrogen receptor modulator. LY117018 TFA exerts antiproliferative effects on breast cancer cell lines[1][2][3]. |
Invitro | LY117018 (0.01-1000 nM;24 h) 在低浓度 (0.01-10 nM) 下,与在剥夺培养基中生长的细胞相比,可使 p53 水平增加,类似于 E2 的作用。在较高浓度的 LY117018 (1 μM) 下,p53 水平似乎下降。用 1 μM LY117018 处理会导致 pRb 主要发生低磷酸化。在低浓度下,LY117018 不会阻止 E2 诱导的 pRb 磷酸化[1]。LY117018 (1 μM;96 h) 抑制 MCF-7 细胞的增殖,其 IC50 为 1 μM[2]。LY117018 通过激活 ERK1/2 信号通路抑制氧化应激诱导的内皮细胞凋亡[3]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> LY117018 TFA 相关抗体: |
CAS | 2390041-98-0 |
Formula | C29H26F3NO6S |
Molar Mass | 573.58 |
Appearance | 固体 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Reference | [1]. Dinda S, et al. Effects of LY117018 (a SERM analog of raloxifene) on tumor suppressor proteins and proliferation of breast cancer cells.Horm Mol Biol Clin Investig. 2010 Aug 1;2(1):211-7. [2]. Baumann KH, et al. Effects of celecoxib and ly117018 combination on human breast cancer cells in vitro.Breast Cancer (Auckl). 2009 Apr 7;3:23-34. [3]. Yu J, et al.Raloxifene analogue LY117018 suppresses oxidative stress-induced endothelial cell apoptosis through activation of ERK1/2 signaling pathway.Eur J Pharmacol. 2008 Jul 28;589(1-3):32-6. |