Buparlisib Hydrochloride

SKU: orb1706891

Description

Buparlisib hydrochloride (BKM120 HCl) is an orally active, pan-class I PI3K inhibitor that acts at nanomolar concentrations. It is widely used in preclinical research to study PI3K pathway dysregulation in various cancers, including breast cancer and glioblastoma, through both in vitro and in vivo experimental models.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1312445-63-8
• MW: 446.85
• Purity: 99.66% (May vary between batches)
• Formula: C₁₈H₂₂ClF₃N₆O₂
• SMILES: Cl.FC(F)(F)C1=CC(=NC=C1C=2N=C(N=C(C2)N3CCOCC3)N4CCOCC4)N
• Target: Apoptosis,PI3K
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.48 mM);DMSO:≥ 40 mg/mL

Bioactivity

• Target IC50:
  p110α-H1047R:58 nM|p110β:166 nM|p110δ:116 nM|Vps34:2.4 μM|mTOR:4.6 μM|p110α:52 nM|p110γ:262 nM|p110α-E545K:99 nM
• In Vivo:
  Methods: Abcg2−/−, Abcb1a/b−/−, and Abcb1a/b;Abcg2−/− mice were treated with Buparlisib Hydrochloride (2 mg/kg, intravenously, 1 hour) to investigate whether P-gp and BCRP could attenuate Buparlisib Hydrochloride brain penetration in vivo. Results: P-gp and BCRP did not limit Buparlisib Hydrochloride brain penetration in vivo. Brain-to-plasma ratios were between 1.5 and 2 for all strains, indicating that Buparlisib Hydrochloride exhibited excellent brain penetration.
• In Vitro:
  MM cell lines were treated with Buparlisib Hydrochloride (10 μM, 24 hours) to observe its effects on cells. Results: Buparlisib Hydrochloride treatment resulted in growth inhibition and apoptosis of MM cells in a dose- and time-dependent manner. The IC50 values for ARP-1, ARK, and MM.1R were between 1 and 10 μM, the IC50 value for MM.1S was <1 μM, and the IC50 value for U266 was between 10 and 100 μM. Buparlisib Hydrochloride treatment resulted in growth inhibition and apoptosis of MM cells in a dose- and time-dependent manner.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Buparlisib Hydrochloride, BKM-120 Hydrochloride, BKM 120 Hydrochloride, BKM120 Hydrochloride, NVP-BKM 120 Hydrochloride, NVP-BKM120 Hydrochloride, NVP-BKM-120 Hydrochloride, p110α, p110γ, p110δ, p110β, p110α-E545K, p110α-H1047R, mTOR, Vps34

Compound Identifiers

PubChem CID

66577015