LY 303511 (hydrochloride)
LY 303511 (hydrochloride) Basic information
- Product Name:
- LY 303511 (hydrochloride)
- Synonyms:
-
- LY 303511 (hydrochloride)
- CS-1207
- 8-Phenyl-2-(piperazin-1-yl)-4H-chromen-4-one hydrochloride
- TNFR,LY-303511,TNF Receptor,inhibit,LY 303511,LY 303511 hydrochloride,Tumor Necrosis Factor Receptor,Inhibitor,Potassium Channel,LY303511,KcsA
- LY 303511 hydrochloride, 10 mM in DMSO
- CAS:
- 2070014-90-1
- MF:
- C19H19ClN2O2
- MW:
- 342.82
- Mol File:
- 2070014-90-1.mol
LY 303511 (hydrochloride) Chemical Properties
- storage temp.
- Inert atmosphere,Room Temperature
- form
- Solid
- color
- White to light yellow
LY 303511 (hydrochloride) Usage And Synthesis
Uses
LY 303511 hydrochloride is a structural analogue of LY294002. LY303511 does not inhibit PI3K. LY303511 enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells. LY303511 reversibly blocks K+ currents (IC50=64.6±9.1 μM) in MIN6 insulinoma cells.
in vivo
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[4].
References
[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. DOI:10.1158/0008-5472.CAN-10-2606
[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. DOI:10.1096/fj.02-0802fje
[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. DOI:10.1158/0008-5472.CAN-08-1996
[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 DOI:10.1124/jpet.105.083550
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