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LY-294002 hydrochloride is a morpholine-containing compound based on the flavonoid quercetin, acting as a potent and cell-permeable PI3K inhibitor, inhibiting PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM in cell-free assays, respectively. It is also an inhibitor of BET (e.g. of BRD2, BRD3, and BRD4). In solution, it is more stable than Wortmannin (PI3K inhibitor). LY294002 is selective against p110α, p110β, p110γ and p110δ, by acting on the ATP binding site of the catalytic subunit of PI3K.
| ln Vitro |
In a dose-dependent manner, LY294002 hydrochloride (0-75 μM; 24 and 48 hours) significantly reduces human nasopharyngeal cancer CNE-2Z cells[4]. LY294002 hydrochloride (0-75 μM; 24 and 48 hours) dose-dependently increases the rate of apoptosis in CNE-2Z cells[4]. In CNE-2Z cells, LY294002 hydrochloride (10–75 μM) dramatically reduces p-Akt (S473) expression levels and increases caspase-9 activity. There is no variation in the total Akt protein level across varied concentrations [4]. Treatment with LY294002 hydrochloride (5, 10, 100 µM; for 2 hours) partially inhibits the nuclear translocation of YAP produced by Lysophosphatidic acid (LPA) (20 µM; for 4 hours), which is followed by a decrease in p-AKT levels[6].
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| ln Vivo |
In a dose-dependent manner, LY294002 hydrochloride (10, 25, 50, 75 mg/kg; ip; twice weekly; for 4 weeks) considerably lowers the mean NPC tumor burden. The effectiveness of LY294002 (10, 25 mg/kg) in reducing tumor burden is lower[4]. In Sprague-Dawley rats, LY294002 hydrochloride (1.2 mg/kg ip; i.p.) for 14 days inhibits the deleterious effects of leptin (60 ug/kg) on spermatozoa[5].
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| Cell Assay |
Cell Proliferation Assay
Cell Types: CNE-2Z cells[4] Tested Concentrations: 0 μM, 10 μM, 25 μM, 50 μM, and 75 μM Incubation Duration: 24 hrs (hours) and 48 hrs (hours) Experimental Results: diminished CNE-2Z cells in a dose-dependent fashion. Apoptosis Analysis Cell Types: CNE-2Z cells[4] Tested Concentrations: 0 μM, 10 μM, 25 μM, 50 μM, and 75 μM Incubation Duration: 24 hrs (hours) and 48 hrs (hours) Experimental Results: Induced apoptosis rate in a dose-dependent manner. Western Blot Analysis Cell Types: CNE-2Z cells[4] Tested Concentrations: 0 μM, 10 μM, 25 μM, 50 μM, and 75 μM Incubation Duration: 24 hrs (hours) and 48 hrs (hours) Experimental Results: diminished phosphorylated Akt (S473) expression levels were Dramatically, up-regulated caspase-9 activity in CNE-2Z cells in treated group. |
| Animal Protocol |
Animal/Disease Models: Athymic nude mice (6-8 weeks) with CNE-2Z xenograft[4]
Doses: 10 mg/kg, 25 mg/kg, 50 mg/kg, and 75 mg/kg Route of Administration: IP; twice weekly, for 4 weeks Experimental Results: Mean Nasopharyngeal carcinoma (NPC) tumor burden was remarkably decreased in a dose-dependent manner. |
| References |
[1]. Bai R, et al. The effect of PI3K inhibitor LY294002 and gemcitabine hydrochloride combined with ionizing radiation on the formation of vasculogenic mimicry of Panc-1 cells in vitro and in vivo. Neoplasma. 2016;63(1):80-92.
[2]. Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007 Jun 15;404(3):449-58. [3]. Gharbi SI, et al. Exploring the specificity of the PI3K family inhibitor LY294002. Biochem J. 2007 May 15;404(1):15-21. [4]. Jiang H, et al. Phosphatidylinositol 3-kinase inhibitor(LY294002) induces apoptosis of human nasopharyngeal carcinoma invitro and in vivo. J Exp Clin Cancer Res. 2010 Apr 22;29:34. [5]. Md Mokhtar AH, et al. LY294002, a PI3K pathway inhibitor, prevents leptin-induced adverse effects on spermatozoa in Sprague-Dawley rats. Andrologia. 2019 Apr;51(3):e13196. [6]. Yi-Jen Hsueh, et al. Lysophosphatidic acid induces YAP-promoted proliferation of human corneal endothelial cells via PI3K and ROCK pathways. Mol Ther Methods Clin Dev. 2015 Apr 29;2:15014. |
| Molecular Formula |
C19H17NO3.HCL
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| Molecular Weight |
343.80412
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| CAS # |
934389-88-5
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| Related CAS # |
LY294002;154447-36-6
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| SMILES |
Cl.O1CCN(C2=CC(=O)C3C=CC=C(C4C=CC=CC=4)C=3O2)CC1
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9087 mL | 14.5433 mL | 29.0867 mL | |
| 5 mM | 0.5817 mL | 2.9087 mL | 5.8173 mL | |
| 10 mM | 0.2909 mL | 1.4543 mL | 2.9087 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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