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Buparlisib Hydrochloride

CAS No. : 1312445-63-8

MCE 站：Buparlisib Hydrochloride

产品活性：Buparlisib Hydrochloride (BKM120 Hydrochloride) 是一种 pan-class I PI3K 抑制剂，作用于p110α/p110β/p110δ/p110γ，IC₅₀ 分别为 52 nM/166 nM/116 nM/262 nM。

研究领域：PI3K/Akt/mTOR  |  Apoptosis

作用靶点：PI3K  |  Apoptosis

In Vitro: Buparlisib (BKM120) exhibits 50-300 nM activity for class I PI3K’s, including the most common p110α mutants. Additionally, NVP-BKM120 exhibits lower potency against class III ａnd class IV PI3K＇s, where 2, 5, >5, ａnd >25 μM biochemical activity is observed for inhibition of VPS34, mTOR, DNAPK, ａnd PI4K, respectively. Buparlisib (BKM120) induces multiple myeloma (MM) cell apoptosis in both dose- ａnd time-dependent manners. Buparlisib (BKM120) at concentrations ≥10 μM induces significant apoptosis in all tested MM cell lines at 24 h (P<0.05, compares with control). Therefore, 10 μM Buparlisib (BKM120) ａnd 24-h treatment are chose in in the following experiments if not stated otherwise. Buparlisib (BKM120) treatment results in a dose-dependent growth inhibition in all tested MM cell lines. Buparlisib (BKM120) IC₅₀ varies among tested MM cells. At 24 h treatment, IC₅₀ for ARP-1, ARK, ａnd MM.1R is between 1 ａnd 10 μM, while IC₅₀ for MM.1S is <1 μM, ａnd IC₅₀ for U266 is between 10 ａnd 100 μM. In summary, Buparlisib (BKM120) treatment results in MM cell growth inhibition ａnd apoptosis in dose- ａnd time-dependent manners.

In Vivo: In A2780 xenograft tumors, oral dosing of Buparlisib (BKM120) at 3, 10, 30, 60, ａnd 100 mg/kg results in a dose dependent modulation of pAKT^Ser473. Partial inhibition of pAKT^Ser473 is observed at 3 ａnd 10 mg/kg, ａnd near complete inhibition is observed at doses of 30, 60, or 100 mg/kg, respectively. Inhibition of pAKT (normalized to total AKT) tracked well with both plasma ａnd tumor drug exposure. Mice receiving Buparlisib (BKM120) (5 μM per kg per day for 15 days) treatment has significantly smaller tumor burdens as compare with control mice, which are measured as tumor volume (P<0.05) ａnd level of circulating human kappa chain (P<0.05). In addition, Buparlisib (BKM120) treatment significantly prolongs the survival of tumor-bearing mice (P<0.05).

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