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LY303511

目录号 M4852 所有产品仅供科研使用,严禁用于人或动物的治疗等任何其他用途,不为任何个人提供产品和服务  


LY303511 is a structural analogue of LY294002, which does not inhibit PI3K, increased homotypic GJIC.

LY303511结构式
包装 价格 库存状态
5mg 原价 ¥ 900
促销价 ¥ 855
中国库存现货
10mg 原价 ¥ 1440
促销价 ¥ 1368
中国库存现货
50mg 原价 ¥ 6120
促销价 ¥ 5814
中国库存现货
其他规格数量报价?

质量控制及产品安全说明书
  • 当前批次:
  • 纯度 >98%
  • COA
  • MSDS
生物活性

LY303511, like rapamycin, inhibited mTOR-dependent phosphorylation of S6K, but not PI3K-dependent phosphorylation of Akt. LY303511 blocked proliferation in A549 as well as in primary pulmonary artery smooth muscle cells, without causing apoptosis. In contrast to rapamycin, LY303511 reduced G(2)/M progression as well as G(2)/M-specific cyclins in A549 cells. Consistent with an additional mTOR-independent kinase target, LY303511 inhibited casein kinase 2 activity, a known regulator of G(1) and G(2)/M progression. In addition to its antiproliferative effect in vitro, LY303511 inhibited the growth of human prostate adenocarcinoma tumor implants in athymic mice. Given its inhibition of cell proliferation via mTOR-dependent and independent mechanisms, LY303511 has therapeutic potential with antineoplastic actions that are independent of PI3K inhibition.

不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
小鼠 大鼠 豚鼠 仓鼠
重量 (kg) 0.02 0.15 1.8 0.4 0.08 10
体表面积 (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km 系数 3 6 12 8 5 20
动物 A (mg/kg) = 动物 B (mg/kg) ×  动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。

化学数据
分子量 306.36
分子式 C19H18N2O2
CAS号 154447-38-8
纯度 >98%
溶解性(25°C) DMSO
储存和运输条件 固体粉末: -20°C 冷藏长期储存
常温运输及临时存放
储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.2641 mL 16.3207 mL 32.6413 mL
5 mM 0.6528 mL 3.2641 mL 6.5283 mL
10 mM 0.3264 mL 1.6321 mL 3.2641 mL
参考文献

Homotypic gap junctional communication associated with metastasis suppression increases with PKA activity and is unaffected by PI3K inhibition.
Bodenstine TM, et al. Cancer Res. 2010 Dec 1;70(23):10002-11. PMID: 21098703.

LY303511 enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells via hydrogen peroxide-mediated mitogen-activated protein kinase activation and up-regulation of death receptors.
Shenoy K, et al. Cancer Res. 2009 Mar 1;69(5):1941-50. PMID: 19223550.

LY303511 (2-piperazinyl-8-phenyl-4H-1-benzopyran-4-one) acts via phosphatidylinositol 3-kinase-independent pathways to inhibit cell proliferation via mammalian target of rapamycin (mTOR)- and non-mTOR-dependent mechanisms.
Kristof AS, et al. J Pharmacol Exp Ther. 2005 Sep;314(3):1134-43. PMID: 15923340.

The phosphatidylinositol 3-kinase inhibitor LY294002 potently blocks K(V) currents via a direct mechanism.
El-Kholy W, et al. FASEB J. 2003 Apr;17(6):720-2. PMID: 12586735.

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关键词:LY303511, LY303511供应商, mTOR抑制剂, 购买LY303511, LY303511结构式

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