| 靶点: |
TRAIL;IC50: 64.6±9.1 µM (K+ currents, in MIN6 insulinoma cells) |
| 体内研究: |
Intraperitoneal administration of vehicle or LY303511 (10 mg/kg/day) is performed when tumors reach a volume of ~150 mm3, 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. |
| 参考文献: |
1. Bodenstine TM, et al. Homotypic gap junctional communication associated with metastasis suppression increases with PKA activity and is unaffected by PI3K inhibition. Cancer Res. 2010 Dec 1;70(23):10002-11. 2. El-Kholy W, Macdonald PE, Lin JH, The phosphatidylinositol 3-kinase inhibitor LY294002 potently blocks K(V) currents via a direct mechanism. FASEB J. 2003 Apr;17(6):720-2. 3. Shenoy K, et al. LY303511 enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells via hydrogen peroxide-mediated mitogen-activated protein kinase activation and up-regulation of death receptors. Cancer Res. 2009 Mar 1;69(5):1941-50. 4. Kristof AS, et al. 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. J Pharmacol E |
| 保存条件: |
RT |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.917 ml |
14.585 ml |
29.17 ml |
| 5 mM |
0.583 ml |
2.917 ml |
5.834 ml |
| 10 mM |
0.292 ml |
1.458 ml |
2.917 ml |
| 50 mM |
0.058 ml |
0.292 ml |
0.583 ml |
|
| 注意: |
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