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LY-294002 hydrochloride

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Purity:99.95%

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COA HNMR HPLC

LY-294002 hydrochloride

Catalog No. T4079Cas No. 934389-88-5

LY-294002 hydrochloride (NSC 697286) is a synthetic molecule inhibitor of PI3Kα/δ/β (IC50: 0.5/0.57/0.97 μM, in cell-free assays); more stable than Wortmannin in solution, and also is a blocker of autophagosome formation.

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Pack Size	Price	Availability
1 mg	$37	In Stock
2 mg	$50	In Stock
5 mg	$68	In Stock
10 mg	$98	In Stock
25 mg	$179	In Stock
50 mg	$298	In Stock
100 mg	$471	In Stock
1 mL x 10 mM (in DMSO)	$68	In Stock

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Product Introduction

Bioactivity

Description	LY-294002 hydrochloride (NSC 697286) is a synthetic molecule inhibitor of PI3Kα/δ/β (IC50: 0.5/0.57/0.97 μM, in cell-free assays); more stable than Wortmannin in solution, and also is a blocker of autophagosome formation.
In vitro	LY294002 inactivates Akt/PKB, consequently inhibiting cell proliferation and inducing apoptosis. In these colon cancer cell lines, LY294002 shows a remarkable growth-inhibitory and apoptosis-inducing effect and decreases expression of phosphorylated Akt (Ser473)[2]. LY294002 induces diminished cytoplasmic volume and obvious nuclear pyknosis in the tumor cells. LY294002 induces specific G1 arrest in cell growth, leading to almost complete inhibition of melanoma cell proliferation and partial inhibition of MG-63 (osteosarcoma cell line) proliferation[3].
In vivo	LY294002 can suppress tumor growth and induce apoptosis, especially in the LoVo tumors. Thus, It shows remarkable effectiveness in the mouse peritonitis carcinoma tosa model [2]. LY294002 markedly inhibits growth and ascites formation of ovarian carcinoma [3].
Kinase Assay	PI3K inhibition by LY294002 is determined in a radiometric assay using purified, recombinant enzymes with 1 μM ATP. The kinase reaction is carried out for 1 hour at room temperature (24oC) and is terminated by addition of PBS. IC50 values are subsequently determined using a sigmoidal dose-response curve fit (variable slope). CK2 and GSK3β (glycogen synthase kinase 3β) inhibition are established by kinase selectivity screening. LY294002 is tested against the Upstate panel of kinases in 10 μM ATP.[4]
Cell Research	Cell lines: Colon cancer cell lines DLD-1,LoVo,HCT15,and Colo205. Concentrations: 0–50 μM. Incubation Time: 0–48 hours. Method: 1.0×105 cells (100 μL volume/well) are inoculated into 96-well microtiter plates.LY294002 is added to triplicate wells and cultured at 37oC for 0–48 hours.After treatment,Premix WST-1 (10 μL) is added to each microculture well,and the plates are incubated for 60 minutes at 37oC,after which absorbance at 450 nm is measured with a microplate reader.[2]
Animal Research	Animal Models: Two groups of athymic nude mice (5–7 weeks) are inoculated i.p.with OVCAR-3 cells. Formulation: Dissolved in DMSO plus 0.25 ml of PBS. Dosages: 0–100 mg/kg. Administration: i.p.[3]
Alias	SF 1101, LY 294002, NSC 697286

Chemical Properties

Molecular Weight	343.81
Formula	C19H17NO3·HCl
Cas No.	934389-88-5

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (145.43 mM)

Ethanol: 5 mM

Solution Preparation Table

DMSO/Ethanol

	1mg	5mg	10mg	50mg
1 mM	2.9086 mL	14.5429 mL	29.0858 mL	145.4292 mL

DMSO

	1mg	5mg	10mg	50mg
5 mM	0.5817 mL	2.9086 mL	5.8172 mL	29.0858 mL
10 mM	0.2909 mL	1.4543 mL	2.9086 mL	14.5429 mL
20 mM	0.1454 mL	0.7271 mL	1.4543 mL	7.2715 mL
50 mM	0.0582 mL	0.2909 mL	0.5817 mL	2.9086 mL
100 mM	0.0291 mL	0.1454 mL	0.2909 mL	1.4543 mL

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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

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LY-294002 hydrochloride

LY-294002 hydrochloride