Buparlisib
Buparlisib (BKM120; NVP-BKM120) is a pan-class I PI3K inhibitor, with IC50s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively.
Product Specifications
CAS Number
[944396-07-0]
Product Name Alternative
BKM120; NVP-BKM120
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Apoptosis; PI3K
Type
Reference compound
Related Pathways
Apoptosis; PI3K/Akt/mTOR
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/NVP-BKM120.html
Concentration
10mM
Purity
99.90
Solubility
DMSO : 100 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 60°C)
Smiles
FC(F)(C1=C(C2=CC(N3CCOCC3)=NC(N4CCOCC4)=N2)C=NC(N)=C1)F
Molecular Formula
C18H21F3N6O2
Molecular Weight
410.39
Precautions
H302, H315, H319, H335
References & Citations
[1]Burger MT, et al. Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer. ACS Med Chem Lett. 2011 Aug 26;2 (10) :774-9.|[2]Zheng Y, et al. Novel phosphatidylinositol 3-kinase inhibitor NVP-BKM120 induces apoptosis in myeloma cells and shows synergistic anti-myeloma activity. J Mol Med (Berl) . 2012 Jun;90 (6) :695-706.|[3]Ni J, et al. Combination inhibition of PI3K and mTORC1 yields durable remissions in mice bearing orthotopic patient-derived xenografts of HER2-positive breast cancer brain metastases. Nat Med. 2016 Jul;22 (7) :723-6.|[4]Liu H, et al. Identifying and Targeting Sporadic Oncogenic Genetic Aberrations in Mouse Models of Triple Negative Breast Cancer. Cancer Discov. 2018 Mar;8 (3) :354-369.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 3
Isoform
PI3Kα; PI3Kβ; PI3Kγ; PI3Kδ; Vps34
Citation 01
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