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- Giri R. Gnawali, .et al. Synthesis of 2-oxoquinoline derivatives as dual pim and mTORC protein kinase inhibitors, Medicinal Chemistry Research, 2022, 31: 1154-1175
- Yusuke Murase, .et al. Antitumor activity of the dual PI3K/mTOR inhibitor gedatolisib and the involvement of ABCB1 in gedatolisib resistance in canine tumor cells, Oncol Rep, 2022, Apr;47(4):61 PMID: 35088890
- Jeremiah J Bearss, .et al. EDC3 phosphorylation regulates growth and invasion through controlling P-body formation and dynamics, EMBO Rep, 2021, Apr 7;22(4):e50835 PMID: 33586867
- Takaaki Fujimura, .et al. Enhanced antitumor effect of alectinib in combination with cyclin-dependent kinase 4/6 inhibitor against RET-fusion-positive non-small cell lung cancer cells, Cancer Biol Ther, 2020, Sep 1;21(9):863-870 PMID: 32835580
- Nachi Namatame, .et al. Antitumor profile of the PI3K inhibitor ZSTK474 in human sarcoma cell lines, Oncotarget, 2018, Oct 12; 9(80): 35141-35161 PMID: 30416685
- Jin H. Song, .et al. Mechanisms Behind Resistance to PI3K Inhibitor Treatment Induced by the PIM Kinase, Mol Cancer Ther, 2018, Dec;17(12):2710-2721 PMID: 30190422
- Saijo A, .et al. Bone marrow-derived fibrocytes promote stem cell-like properties of lung cancer cells, Cancer Lett, 2018, May 1;421:17-27 PMID: 29448000
- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Pridham KJ, .et al. PIK3CB/p110β is a selective survival factor for glioblastoma, Neuro Oncol, 2018, Mar 27;20(4):494-505 PMID: 29016844
- Charles-André Philip, .et al. Inhibition of PI3K-AKT-mTOR pathway sensitizes endometrial cancer cell lines to PARP inhibitors, BMC Cancer, 2017, 17: 638 PMID: 28886696
- Rogers HA, .et al. PI3K pathway activation provides a novel therapeutic target for pediatric ependymoma and is an independent marker of progression-free survival., Clin Cancer Res., 2013, Dec 1;19(23):6450-60 PMID: 24077346
Biological Activity
BKM120 (NVP-BKM120) is a bioavailable specific oral pan-class I phosphatidylinositol 3-kinase (PI3K) kinase inhibitor.
Targets
| Target | Value |
|---|---|
| p110α | IC50: 52nM |
| p110δ | IC50: 116nM |
| p110β | IC50: 166nM |
| p110γ | IC50: 262nM |
| Vps34 | IC50: 2.4μM |
| mTOR | IC50: 4.6μM |
| DNA-PK | IC50: >5μM |
| PI4Kβ | IC50: >25μM |
| In vitro (25°C) | DMSO | 76 mg/mL (185.18 mM) | |
| Water | Insoluble | ||
| Ethanol | 2 mg/mL (4.87 mM) | ||
| In vivo | 5% DMSO+30% PEG 300+ddH2O | 14 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 24.37 mL | 121.83 mL | 243.66 mL |
| 0.5 mM | 4.87 mL | 24.37 mL | 48.73 mL |
| 1 mM | 2.44 mL | 12.18 mL | 24.37 mL |
| 5 mM | 0.49 mL | 2.44 mL | 4.87 mL |
*The above data is based on the productmolecular weight 410.4 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A11016 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 944396-07-0 |
| Formula | C18H21F3N6O2 |
| M. Wt | 410.4 |
| Purity | >98% |
| SMILES | C1COCCN1C2=NC(=NC(=C2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4 |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
Datasheet
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