Omipalisib

Name: Omipalisib
Brand: Tocris Bioscience
SKU: 6792

Tocris Bioscience, part of Bio-Techne | Catalog # 6792

COA / SDS

Highly potent PI 3-kinase inhibitor; also potent inhibitor of mTOR and DNA-PK

Key Product Details

Description:	Highly potent PI 3-kinase inhibitor; also potent inhibitor of mTOR and DNA-PK
Alternative Names:	GSK2126458
Chemical Name:	2,4-Difluoro-N-[2-methoxy-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl]benzenesulfonamide
Purity:	≥98% (HPLC)
Molecular Weight:	505.5

View Full Technical Details for Omipalisib

Technical Data
Citations

Biological Activity for Omipalisib

Omipalisib is a highly potent PI 3-K inhibitor (IC₅₀ = 0.04 nM). Also inhibits mTOR (K_i = 0.18 - 0.3 nM) and DNA-PK (IC₅₀ = 0.28 nM). Induces G₁ cell cycle arrest and inhibits proliferation of some breast cancer cells lines in vitro. Reduces pAKT-S473 levels in and inhibits growth of BT474 breast cancer xenografts in mice. Orally bioavailable.

Compound Libraries for Omipalisib

Omipalisib is also offered as part of the Tocriscreen Kinase Inhibitor Library and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for Omipalisib

M. Wt	505.5
Formula	C₂₅H₁₇F₂N₅O₃S
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1086062-66-9
PubChem ID	25167777
InChi Key	CGBJSGAELGCMKE-UHFFFAOYSA-N
Smiles	COC1=NC=C(C2=CC3=C(N=CC=C3C4=CN=NC=C4)C=C2)C=C1NS(=O)(C5=C(C=C(C=C5)F)F)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Omipalisib

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	10.11	20

Preparing Stock Solutions for Omipalisib

The following data is based on the product molecular weight 505.5.

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
0.2 mM	9.89 mL	49.46 mL	98.91 mL
1 mM	1.98 mL	9.89 mL	19.78 mL
2 mM	0.99 mL	4.95 mL	9.89 mL
10 mM	0.20 mL	0.99 mL	1.98 mL

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Reconstitution Calculator

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References for Omipalisib

References are publications that support the biological activity of the product.

Knight Discovery of GSK2126458, a highly potent inhibitor of PI3K and the mammalian target of rapamycin. ACS Med.Chem.Lett. 2010 PMID: 24900173