BKM120 (NVP-BKM120, Buparlisib) Property

Melting point:

143-147°C

Boiling point:

645.7±65.0 °C(Predicted)

Density 

1.382

storage temp. 

-20°C

solubility 

Soluble in DMSO (15 mg/ml)

form 

White powder.

pka

5.94±0.50(Predicted)

color 

White

Stability:

Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

Safety

HS Code 

29349990

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H301Toxic if swalloed

H341Suspected of causing genetic defects

H372Causes damage to organs through prolonged or repeated exposure

Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P281Use personal protective equipment as required.

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

P308+P313IF exposed or concerned: Get medical advice/attention.

P314Get medical advice/attention if you feel unwell.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P405Store locked up.

P501Dispose of contents/container to..…

BKM120 (NVP-BKM120, Buparlisib) Chemical Properties,Usage,Production

Description

Buparlisib (944396-07-0) is potent pan-Class I PI3-kinase inhibitor (IC50’s: p110α = 52 nM, p110? = 166 nM, p110δ = 116 nM. P110g = 262 nM).1,2 It inhibited microtubule dynamics at in vitro concentrations >1μM and doses above 50mg/kg in mice.3 Buparlisib lead to a precipitous drop in DNA synthesis in a mouse model of BRCA1-linked triple-negative breast cancer with less affect in normal tissue.4

Uses

A selective Class I PI3K inhibitor of p110α, p110β, p110δ and p110γ with IC50s of 50-300 nM.

Uses

NVP-BKM 120 is 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

ChEBI: BKM120 is an aminopyridine that is 4-(trifluoromethyl)pyridin-2-amine substituted at position 5 by a 2,6-di(morpholin-4-yl)pyrimidin-4-y group. A selective PI3K inhibitor with anti-tumour properties. It has a role as an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor and an antineoplastic agent. It is a member of morpholines, an aminopyrimidine, an aminopyridine and an organofluorine compound.

target

p110α

References

Burger et al. (2011), Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer; ACS Med. Chem. Lett. 2 774 Maira et al. (2012), Identification and Characterization of NVP-BKM120, an Orally Available Pan-Class I PI3-Kinase Inhibitor; Mol. Cancer Ther. 11 317 Brachmann et al. (2012), Characterization of the mechanism of action of the pan class I PI3K inhibitor NVP-BKM120 across a broad range of concentrations; Mol. Cancer Ther. 11 1747 Juvekar et al. (2016), Phosphoinositide 3-kinase inhibitors induce DNA damage through nucleoside depletion; Proc. Natl. Acad. Sci USA. 113 E4338