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NVP-BKM120
- BKM 120 - Buparlisib
- Soluble in DMSO
- MF: C18H21F3N6O2
- MW: 410.39
Description
NVP-BKM120 (Buparlisib) is a potent, selective and orally bioavailable class I phosphoinositide 3-kinase (PI3K) inhibitor with IC50 values of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ isoforms, respectively. Buparlisib is highly permeable to the blood-brain barrier (BBB) to disrupt the oncogenic PI3K-AKT-mTOR signaling.
Class I PI3Ks regulate survival, proliferation, metabolism and therapeutic resistance in many tumor models. NVP-BKM120 is used to interrogate PI3K-dependent signaling and evaluate pathway inhibition in cancer and cell-survival assays.
Key Features
- Pan-class I PI3K inhibitor
- Targets PI3K-driven AKT-mTOR pathway signaling
- Orally bioavailable oncology-relevant research compound
- Useful for evaluating PI3K-dependent survival and proliferation
Applications
- PI3K-AKT-mTOR pathway studies
- Cancer cell survival and proliferation assays
- PI3K inhibitor sensitivity and resistance profiling
- Signal transduction and pharmacodynamic biomarker research
More Information
| Parent CAS No. | 944396-07-0 |
|---|---|
| Chemical Name | 5-(2,6-dimorpholinopyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine |
| SMILES | C1C(N2CCOCC2)=NC(N2CCOCC2)=NC=1C1C=NC(N)=CC=1C(F)(F)F |
| MFCD | N.A. |
| InChi | InChI=1S/C18H21F3N6O2/c19-18(20,21)13-9-15(22)23-11-12(13)14-10-16(26-1-5-28-6-2-26)25-17(24-14)27-3-7-29-8-4-27/h9-11H,1-8H2,(H2,22,23) |
| InChiKey | CWHUFRVAEUJCEF-UHFFFAOYSA-N |
| CID | 16654980 |
| Short Description | PI3K inhibitor |
References
- CW Lindsley et al. (3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu5: discovery of a new tool compound with activity in the OSS mouse model of addiction. ACS Chem. Neurosci. 2011, 2(8), 471-482.
- D Koul et al. Antitumor activity of NVP-BKM120--a selective pan class I PI3 kinase inhibitor showed differential forms of cell death based on p53 status of glioma cells. Clin Cancer Res. 2012, 18(1), 184-195.
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