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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)

Biological Activity for Omipalisib

Omipalisib is a highly potent PI 3-K inhibitor (IC50 = 0.04 nM). Also inhibits mTOR (Ki = 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
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 Data for Omipalisib

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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 0.2 mL 0.99 mL 1.98 mL

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References for Omipalisib

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

Knight et al (2010) Discovery of GSK2126458, a highly potent inhibitor of PI3K and the mammalian target of rapamycin. ACS Med.Chem.Lett. 1 39 PMID: 24900173

If you know of a relevant reference for Omipalisib, please let us know.

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Citations for Omipalisib

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