Synonym
LY294002,4'-NH2; PI-828; PI 828; PI828.
IUPAC/Chemical Name
8-(4-aminophenyl)-2-(4-morpholinyl)-4H-1-benzopyran-4-one
InChi Key
WUKMIBOGGXMBAC-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H18N2O3/c20-14-6-4-13(5-7-14)15-2-1-3-16-17(22)12-18(24-19(15)16)21-8-10-23-11-9-21/h1-7,12H,8-11,20H2
SMILES Code
O=C1C=C(N2CCOCC2)OC3=C(C4=CC=C(N)C=C4)C=CC=C13
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
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
Biological target:
PI-828 is a dual PI3K and casein kinase 2 (CK2) inhibitor with IC50s of 173 nM, 149 nM, and 1127 nM for p110α, CK2, and CK2α2 in lipid kinase assay.
In vitro activity:
The anti-tumour effects of PI3K inhibitors (PI-828, PI-103 and PX-866) in terms of cell proliferation, colony formation, induction of apoptosis, cell cycle arrest, invasion, autophagy, and pNF-κB/p65 translocation in SCC-4, SCC-9 and SCC-25 cells were studied by performing MTT, clonogenic, DAPI staining, propidium iodide staining, annexin-V binding, matrigel invasion, acridine orange staining and immuno-fluorescence assay. PI-828 and PI-103 treatment exhibited dose-dependent inhibition of growth and proliferation of OSCC cells with a concomitant induction of apoptosis, altered cell cycle regulation and decreased invasiveness (p < 0.01).
Reference: Cancer Chemother Pharmacol. 2019 Mar;83(3):451-461. https://pubmed.ncbi.nlm.nih.gov/30519710/
|
Solvent |
mg/mL |
mM |
comments |
| Solubility |
| DMF |
25.0 |
77.55 |
|
| DMSO |
23.3 |
72.11 |
|
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
322.36
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:
Aggarwal S, John S, Sapra L, Sharma SC, Das SN. Targeted disruption of PI3K/Akt/mTOR signaling pathway, via PI3K inhibitors, promotes growth inhibitory effects in oral cancer cells. Cancer Chemother Pharmacol. 2019 Mar;83(3):451-461. doi: 10.1007/s00280-018-3746-x. Epub 2018 Dec 5. PMID: 30519710.
In vitro protocol:
Aggarwal S, John S, Sapra L, Sharma SC, Das SN. Targeted disruption of PI3K/Akt/mTOR signaling pathway, via PI3K inhibitors, promotes growth inhibitory effects in oral cancer cells. Cancer Chemother Pharmacol. 2019 Mar;83(3):451-461. doi: 10.1007/s00280-018-3746-x. Epub 2018 Dec 5. PMID: 30519710.
1: Agosto-Marlin IM, Nikodemova M, Dale EA, Mitchell GS. BDNF-induced phrenic motor facilitation shifts from PKCθ to ERK dependence with mild systemic inflammation. J Neurophysiol. 2023 Feb 1;129(2):455-464. doi: 10.1152/jn.00345.2022. Epub 2023 Jan 25. PMID: 36695529; PMCID: PMC9942899.
2: Aggarwal S, John S, Sapra L, Sharma SC, Das SN. Targeted disruption of PI3K/Akt/mTOR signaling pathway, via PI3K inhibitors, promotes growth inhibitory effects in oral cancer cells. Cancer Chemother Pharmacol. 2019 Mar;83(3):451-461. doi: 10.1007/s00280-018-3746-x. Epub 2018 Dec 5. PMID: 30519710.
3: Agosto-Marlin IM, Mitchell GS. Spinal BDNF-induced phrenic motor facilitation requires PKCθ activity. J Neurophysiol. 2017 Nov 1;118(5):2755-2762. doi: 10.1152/jn.00945.2016. Epub 2017 Aug 30. PMID: 28855298; PMCID: PMC5675902.
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6: Hoffman MS, Nichols NL, Macfarlane PM, Mitchell GS. Phrenic long-term facilitation after acute intermittent hypoxia requires spinal ERK activation but not TrkB synthesis. J Appl Physiol (1985). 2012 Oct 15;113(8):1184-93. doi: 10.1152/japplphysiol.00098.2012. Epub 2012 Sep 6. PMID: 22961271; PMCID: PMC3472488.
7: Zellefrow CD, Sharlow ER, Epperly MW, Reese CE, Shun T, Lira A, Greenberger JS, Lazo JS. Identification of druggable targets for radiation mitigation using a small interfering RNA screening assay. Radiat Res. 2012 Sep;178(3):150-9. doi: 10.1667/rr2810.1. Epub 2012 Jul 2. PMID: 22747550; PMCID: PMC4528675.
8: Saleh SN, Albert AP, Large WA. Activation of native TRPC1/C5/C6 channels by endothelin-1 is mediated by both PIP3 and PIP2 in rabbit coronary artery myocytes. J Physiol. 2009 Nov 15;587(Pt 22):5361-75. doi: 10.1113/jphysiol.2009.180331. Epub 2009 Sep 21. PMID: 19770190; PMCID: PMC2788089.
