Buparlisib Hydrochloride Chemical Properties

storage temp. 

Store at -20°C

solubility 

≥44.7 mg/mL in DMSO; ≥52.8 mg/mL in H2O with gentle warming; ≥96 mg/mL in EtOH with gentle warming

form 

solid

color 

White to yellow

InChI

InChI=1S/C18H21F3N6O2.ClH/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);1H

InChIKey

DGPLYAXBXJXEID-UHFFFAOYSA-N

SMILES

C(C1=CC(N)=NC=C1C1=NC(N2CCOCC2)=NC(N2CCOCC2)=C1)(F)(F)F.Cl

Buparlisib Hydrochloride Usage And Synthesis

Uses

NVP-BKM 120-d16 Hydrochloride is the salt, labeled analogue of NVP-BKM 120 (N925760), a novel anti-tumor active compound that is selective in that it inhibits specifically PI3 kinase activating cell death in glioma cells. Glioma cells being those that proliferate from tumors in the brain or the spine.

Definition

Buparlisib hydrochloride (BKM120 Hydrochloride) is an investigational small molecule orally available pan-class I phosphoinositide 3-kinase inhibitor, with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/p110β/p110δ/p110γ, respectively.

Mode of action

Buparlisib specifically inhibits class I PIK3 in the PI3K/AKT kinase signaling pathway in an ATP-competitive manner, thus inhibiting the production of the secondary messenger phosphatidylinositol (3,4,5)-trisphosphate and activation of the PI3K signaling pathway. This may induce inhibition of tumour cell growth and survival in susceptible tumour cell populations. Buparlisib is currently under investigation in patients with a variety of solid tumours, including breast cancer[1].

References

[1] Carmen Criscitiello. “Profile of buparlisib and its potential in the treatment of breast cancer: evidence to date.” Breast Cancer?: Targets and Therapy 10 (2018): 23–29.

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