LY303511 free base | NV-128 | CAS#154447-38-8 | 854127-90-5 | 2070014-90-1 | mTOR inhibitor

LY303511
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 407219

CAS#: 154447-38-8 (free base)

Description: LY303511, also known as NV-128 and EM 101, is a potent mTOR inhibitor. LY303511 enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells via hydrogen peroxide-mediated mitogen-activated protein kinase activation and up-regulation of death receptors. LY303511 amplifies TRAIL-induced apoptosis in tumor cells by enhancing DR5 oligomerization, DISC assembly, and mitochondrial permeabilization. LY303511 acts via phosphatidylinositol 3-kinase-independent pathways to inhibit cell proliferation via mammalian target of rapamycin (mTOR)- and non-mTOR-dependent mechanisms.

Chemical Structure

LY303511

CAS# 154447-38-8 (free base)

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 407219
Name: LY303511
CAS#: 154447-38-8 (free base)
Chemical Formula: C19H18N2O2
Exact Mass: 306.14
Molecular Weight: 306.365
Elemental Analysis: C, 74.49; H, 5.92; N, 9.14; O, 10.44

Price and Availability

Size	Price	Availability
5mg	USD 300	2 Weeks
10mg	USD 550	2 Weeks
25mg	USD 950	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Related CAS #: 854127-90-5 (2HCl) 2070014-90-1 (HCl) 154447-38-8 (free base)

Synonym: LY303511; LY-303511; LY 303511; NV-128; NV 128; NV128; EM 101; EM-101; EM101.

IUPAC/Chemical Name: 2-(1-Piperazinyl)-8-phenyl-4H-1-benzopyran-4-one

InChi Key: NGAGMBNBKCDCDJ-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H18N2O2/c22-17-13-18(21-11-9-20-10-12-21)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13,20H,9-12H2

SMILES Code: O=C1C=C(N2CCNCC2)OC3=C(C4=CC=CC=C4)C=CC=C13

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:

Product Data

Instruction:

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Biological target:	LY303511, also known as NV-128 and EM 101, is a potent mTOR inhibitor.
In vitro activity:	LY303511 (LY30), an inactive analogue of LY29, also inhibited MCP-1 expression. LY29 and LY30 inhibited activation of nuclear factor-kappaB (NF-kappaB). These results suggest that LY29 inhibits MCP-1 expression at least in part via suppression of NF-kappaB, independent of PI3K, and the structure of LY29 and LY30 may be a novel template for development of new anti-inflammatory drugs. Reference: FEBS Lett. 2004 Feb 13;559(1-3):141-4. https://pubmed.ncbi.nlm.nih.gov/14960322/
In vivo activity:	In 8-oxo-2'-deoxyguanosine assay, LY303511 induces oxidative DNA damage in oral cancer cells. In zebrafish model, LY303511 inhibits CAL 27-xenografted tumor growth. Therefore, LY303511 displays antiproliferation potential against oral cancer cells in vitro and in vivo. Reference: Environ Toxicol. 2019 Aug;34(8):958-967. https://pubmed.ncbi.nlm.nih.gov/31115172/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	30.6	100.00

Preparing Stock Solutions

The following data is based on the product molecular weight 306.37 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	1. Choi EK, Park HJ, Ma JS, Lee HC, Kang HC, Kim BG, Kang IC. LY294002 inhibits monocyte chemoattractant protein-1 expression through a phosphatidylinositol 3-kinase-independent mechanism. FEBS Lett. 2004 Feb 13;559(1-3):141-4. doi: 10.1016/S0014-5793(04)00058-4. PMID: 14960322. 2. El-Kholy W, Macdonald PE, Lin JH, Wang J, Fox JM, Light PE, Wang Q, Tsushima RG, Wheeler MB. 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. Epub 2003 Feb 5. PMID: 12586735. 3. Tang JY, Xu YH, Lin LC, Ou-Yang F, Wu KH, Tsao LY, Yu TJ, Huang HW, Wang HR, Liu W, Chang HW. LY303511 displays antiproliferation potential against oral cancer cells in vitro and in vivo. Environ Toxicol. 2019 Aug;34(8):958-967. doi: 10.1002/tox.22767. Epub 2019 May 21. PMID: 31115172.
In vitro protocol:	1. Choi EK, Park HJ, Ma JS, Lee HC, Kang HC, Kim BG, Kang IC. LY294002 inhibits monocyte chemoattractant protein-1 expression through a phosphatidylinositol 3-kinase-independent mechanism. FEBS Lett. 2004 Feb 13;559(1-3):141-4. doi: 10.1016/S0014-5793(04)00058-4. PMID: 14960322. 2. El-Kholy W, Macdonald PE, Lin JH, Wang J, Fox JM, Light PE, Wang Q, Tsushima RG, Wheeler MB. 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. Epub 2003 Feb 5. PMID: 12586735.
In vivo protocol:	1. Tang JY, Xu YH, Lin LC, Ou-Yang F, Wu KH, Tsao LY, Yu TJ, Huang HW, Wang HR, Liu W, Chang HW. LY303511 displays antiproliferation potential against oral cancer cells in vitro and in vivo. Environ Toxicol. 2019 Aug;34(8):958-967. doi: 10.1002/tox.22767. Epub 2019 May 21. PMID: 31115172.

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1: Shi Y, Mellier G, Huang S, White J, Pervaiz S, Tucker-Kellogg L. Computational modelling of LY303511 and TRAIL-induced apoptosis suggests dynamic regulation of cFLIP. Bioinformatics. 2013 Feb 1;29(3):347-54. doi: 10.1093/bioinformatics/bts702. Epub 2012 Dec 13. PubMed PMID: 23239672; PubMed Central PMCID: PMC3562069.

2: Tucker-Kellogg L, Shi Y, White JK, Pervaiz S. Reactive oxygen species (ROS) and sensitization to TRAIL-induced apoptosis, in Bayesian network modelling of HeLa cell response to LY303511. Biochem Pharmacol. 2012 Nov 15;84(10):1307-17. doi: 10.1016/j.bcp.2012.08.028. Epub 2012 Sep 6. PubMed PMID: 22982511.

3: Shenoy K, Wu Y, Pervaiz S. 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. Epub 2009 Feb 17. Erratum in: Cancer Res. 2012 Jan 1;72(1):375. PubMed PMID: 19223550.

4: Poh TW, Huang S, Hirpara JL, Pervaiz S. LY303511 amplifies TRAIL-induced apoptosis in tumor cells by enhancing DR5 oligomerization, DISC assembly, and mitochondrial permeabilization. Cell Death Differ. 2007 Oct;14(10):1813-25. Epub 2007 Jun 22. PubMed PMID: 17585340.

5: Poh TW, Pervaiz S. LY294002 and LY303511 sensitize tumor cells to drug-induced apoptosis via intracellular hydrogen peroxide production independent of the phosphoinositide 3-kinase-Akt pathway. Cancer Res. 2005 Jul 15;65(14):6264-74. PubMed PMID: 16024628.

6: Kristof AS, Pacheco-Rodriguez G, Schremmer B, Moss J. 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 Exp Ther. 2005 Sep;314(3):1134-43. Epub 2005 May 27. PubMed PMID: 15923340.

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