BKM120 (NVP-BKM120, Buparlisib)

Bezeichnung:BKM120 (NVP-BKM120, Buparlisib)

CAS-Nr944396-07-0

Englisch Name:BKM120 (NVP-BKM120, Buparlisib)

CBNumberCB82509983

SummenformelC18H21F3N6O2

Molgewicht410.39

MOL-Datei944396-07-0.mol

BKM120 (NVP-BKM120, Buparlisib) physikalisch-chemischer Eigenschaften

Schmelzpunkt	143-147°C
Siedepunkt	645.7±65.0 °C(Predicted)
Dichte	1.382
storage temp.	-20°C
Löslichkeit	Soluble in DMSO (15 mg/ml)
Aggregatzustand	White powder.
pka	5.94±0.50(Predicted)
Farbe	White
Stabilität	Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

Sicherheit

HS Code

29349990

Gefahreninformationscode (GHS)

BKM120 (NVP-BKM120, Buparlisib) Chemische Eigenschaften,Einsatz,Produktion Methoden

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

BKM120 (NVP-BKM120, Buparlisib) Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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