化学信息：
|
化学名
|
8-phenyl-2-piperazin-1-ylchromen-4-one
|
|
|
简称
|
LY303511
|
|
别名
|
LY-303511, LY303511
|
|
中文名
|
N/A
|
|
化学式
|
C19H18N2O2
|
|
分子量
|
306.36
|
|
CAS号
|
154447-38-8
|
|
纯度
|
98%
|
|
溶剂/溶解度
|
Water<1mg/ml; DMSO30.6mg/ml; Ethanol<1mg/ml
|
|
溶液配制
|
5mg加入1.63ml DMSO，或者每3.06mg加入1ml DMSO，配制成10mM溶液。SF2816-10mM用DMSO配制。
|
生物信息：
|
产品描述
|
LY303511, an inactive analogue of LY294002, is a mTOR inhibitor that did not inhibit PI3-K.
|
|
信号通路
|
PI3K/Akt/mTOR
|
|
靶点
|
－
|
－
|
－
|
－
|
－
|
|
IC50
|
－
|
－
|
－
|
－
|
－
|
|
体外研究
|
100μM LY303511 significantly reduced the fraction of cells in S phase. The proportion of cells in G2/M remained unchanged, indicating that cells were arrested in both G1 and G2/M. In contrast, rapamycin increased the G1 population by reducing the proportion of cells in both S and G2/M. The effects of 10μM LY303511 and rapamycin on the reduction in S phase cells were additive to that of 10μM LY303511 alone (P=0.056). In MIN6 insulinoma cells, wortmannin (100nM) had no effect on whole-cell outward K+ currents, but LY294002 and LY303511 reversibly blocked currents in a dose-dependent manner (IC50=9.0+/-0.7mM and 64.6+/-9.1mM, respectively). Western blotting confirmed the specific inhibitory effects of LY294002 and wortmannin on insulin-stimulated PI3K activity. Both LY294002 and LY303511 increased the activity of protein kinase A (PKA). Moreover, PKA blockade by the small molecule inhibitor H89 decreased the LY294002/LY303511-mediated increase in GJIC.
|
|
体内研究
|
PND4 ovaries were cultured for 8 days in control medium or medium containing VCD (30μM) in the presence or absence of LY303511 (20μM). Incubation with LY303511 alone caused a reduction (P<0.05) in primordial and small primary follicle numbers. On the other hand, whereas VCD alone depleted (P<0.05) primordial and small primary follicle numbers, this depletion was not prevented by co-incubation with LY303511.
|
|
临床实验
|
N/A
|
|
特征
|
N/A
|
相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
|
酶活性检测实验
|
|
方法
|
N/A
|
|
细胞实验
|
|
细胞系
|
N/A
|
|
浓度
|
N/A
|
|
处理时间
|
N/A
|
|
方法
|
N/A
|
|
动物实验
|
|
动物模型
|
N/A
|
|
配制
|
N/A
|
|
剂量
|
N/A
|
|
给药方式
|
N/A
|
参考文献：
1. Kristof AS, Pacheco-Rodriguez G, Schremmer B. J Pharmacol Exp Ther. 2005 Sep, 314(3), 1134-43.
2. El-Kholy W, Macdonald PE, Lin JH. FASEB J. 2003 Apr, 17(6), 720-2.
3. Bodenstine TM, Vaidya KS, Ismail A. Cancer Res. 2010 Dec 1, 70(23), 10002-11.
4. Keating AF, J Mark C, Sen N. Toxicol Appl Pharmacol. 2009 Dec 1, 241(2), 127-34.
包装清单：
|
产品编号
|
产品名称
|
包装
|
|
SF2816-10mM
|
LY303511 (mTOR抑制剂)
|
10mM×0.2ml
|
|
SF2816-5mg
|
LY303511 (mTOR抑制剂)
|
5mg
|
|
SF2816-25mg
|
LY303511 (mTOR抑制剂)
|
25mg
|
|
—
|
说明书
|
1份
|
保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
注意事项：
本产品仅限于专业人员的科学研究用，不得用于临床诊断或治疗，不得用于食品或药品，不得存放于普通住宅内。
为了您的安全和健康，请穿实验服并戴一次性手套操作。
微信在线咨询
微信在线咨询
