| Name | Buparlisib Hydrochloride |
| Description | Buparlisib Hydrochloride (BKM120 HCl) is a specific and orally bioavailable pan-class I PI3K inhibitor that competitively inhibits PI3K/AKT kinase at the nanomolar level and suppresses cancer cell growth, making it suitable for studying breast cancer, glioblastoma, and solid tumours. |
| 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. [2] |
| 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. [3] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.48 mM), Sonication is recommended. DMSO : ≥ 40 mg/mL, Sonication is recommended.
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| Keywords | Vps34 | p110δ | p110γ | p110β | p110α-H1047R | p110α-E545K | p110α | NVP-BKM-120 Hydrochloride | NVP-BKM 120 Hydrochloride | mTOR | Buparlisib Hydrochloride | BKM-120 Hydrochloride | BKM 120 Hydrochloride |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Formamide | Dimethyl phthalate | Alginic acid | Sodium Molybdate | Sildenafil citrate |
| Related Compound Libraries | PI3K-AKT-mTOR Compound Library | Bioactive Compound Library | Immunology/Inflammation Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |