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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 |
| 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 Data for Omipalisib
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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 | 0.2 mL | 0.99 mL | 1.98 mL |
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Product Datasheets for Omipalisib
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
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Keywords: Omipalisib, Omipalisib supplier, PI, 3-Kinase, PI3K, mTOR, DNA-PK, highly, potent, inhibitors, inhibits, orally, bioavailable, anticancer, GSK2126458, DNA-dependent, Protein, Kinase, 6792, Tocris Bioscience
Citations for Omipalisib
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