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8-苯基-2-(1-哌嗪基)-4H-1-苯并吡喃-4-酮

8-苯基-2-(1-哌嗪基)-4H-1-苯并吡喃-4-酮

英文名称:LY 303511
CAS号:154447-38-8
分子式:C19H18N2O2
分子量:306.36
EINECS号:
Mol文件:154447-38-8.mol
8-苯基-2-(1-哌嗪基)-4H-1-苯并吡喃-4-酮 结构式

8-苯基-2-(1-哌嗪基)-4H-1-苯并吡喃-4-酮 性质

沸点 496.1±45.0 °C(Predicted)
密度 1.237±0.06 g/cm3(Predicted)
储存条件 Store at +4°C
溶解度 1eq 中可溶解至 100 mM。 HCl 和 DMSO 中浓度为 100 mM
形态 琥珀色固体
酸度系数(pKa) 9.20±0.10(Predicted)

8-苯基-2-(1-哌嗪基)-4H-1-苯并吡喃-4-酮 用途与合成方法

LY303511 是 LY294002 的一种结构类似物,但 LY303511 不抑制 PI3K。LY303511 可增强 SHEP-1 神经母细胞瘤细胞的TRAIL 敏感性。LY303511 可逆地阻断 MIN6 胰岛瘤细胞中的 K+ 电流 (IC50=64.6±9.1 μM)。

TRAIL
IC50: 64.6±9.1 µM (K + currents, in MIN6 insulinoma cells)

LY303511 is structurally identical to LY294002 except for a substitution of -O for -NH in the morpholine ring, and does not potently inhibit PI3K. Treatment of cells with LY303511 causes an increase in calcein spread similar to levels of LY294002. The ability of LY303511 to increase gap junctional intercellular communication (GJIC) does not occur concomitant with inhibition of phosphorylation of AKT as measured by immunoblotting. LY303511 enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells via H 2 O 2 -MAPK activation and up-regulation of death receptors. SHEP-1 cells are exposed to varying concentrations of LY303511 (LY30), TRAIL, and a combination of the two (1 h preincubation with LY303511 followed by TRAIL for 4 hours). SHEP-1 cells are responsive to TRAIL (~10%, ~15%, and ~30% reduction in the surviving fraction at 25, 50, and 100 ng/mL, respectively); however, treatment with LY303511 (12.5, 25, or 50 μM) has no effect on cell viability. However, incubation of cells with LY303511 (25 μM) for 1 hour followed by 4 hours exposure to 50 ng/mL of TRAIL has a strong synergistic effect (~40% reduction in viable cells with LY303511+TRAIL versus ~15% with TRAIL alone). LY303511 is a negative control compound with respect to PI3K activity. In MIN6 insulinoma cells, Wortmannin (100 nM) has no effect on whole-cell outward K + currents, but LY294002 and LY303511 reversibly block currents in a dose-dependent manner (IC 50 =9.0±0.7 μM and 64.6±9.1 μM, respectively). Kv2.1 and Kv1.4 are highly expressed in beta-cells, and in Kv2.1-transfected tsA201 cells, 50 μM LY294002 and 100 μM LY303511 reversibly inhibit currents by 99% and 41%, respectively. LY303511 blocks currents with an IC 50 of 64.6±9.1 µM, with a maximal inhibition of ~90% at 500 µM (n≥5 cells at each concentration).

Intraperitoneal administration of vehicle or LY303511 (10 mg/kg/day) is performed when tumors reach a volume of ~150 mm 3 , at which time 35 mice have developed a tumor. After 21 days, >15% of the mice require euthanasia because of excessive tumor growth, and these data are censored due to unreliable estimates of average tumor volume. The administration of LY303511, 10 mg/kg/day, is sufficient to inhibit PC-3 tumor growth in vivo.

8-苯基-2-(1-哌嗪基)-4H-1-苯并吡喃-4-酮供应商 更多

武汉易泰科技有限公司上海分公司
联系电话:821-50328103-801 18930552037
产品介绍:
英文名称:LY 303511;2-(1-Piperazinyl)-8-phenyl-4H-1-benzopyran-4-one
CAS:154447-38-8
纯度:99% HPLC
包装信息:1Mg ; 5Mg;10Mg ;100Mg;250Mg ;500Mg ;1g;2.5g ;5g ;10g
上海楼岚生物科技有限公司
联系电话:021-52996696,15000506266 15000506266
产品介绍:
英文名称:LY303511
CAS:154447-38-8
上海一飞生物科技有限公司
联系电话:021-65675885 18964387627
产品介绍:
英文名称:LY 303511
CAS:154447-38-8
纯度:95%
包装信息:1mg;5mg;10mg
备注:试剂级
上海瀚香生物科技有限公司
联系电话:177-54423994 17754423994
产品介绍:
英文名称:LY 303511
CAS:154447-38-8
纯度:98% HPLC LCMS
包装信息:100mg;500mg;1g;5g;10g
备注:量大优惠,现货促销
上海巢莱化工科技中心
联系电话:021-2022843681 15618226720
产品介绍:
英文名称:LY 303511
CAS:154447-38-8
纯度:95%
包装信息:1G,5G,10G,50G,100G,1KG

最新发布供应信息

化合物 LY 303511|T2434|TargetMol
TargetMol中国(陶术生物) 2024-12-12

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