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| Cas No.: | 944396-07-0 |
| Chemical Name: | Buparlisib (BKM120) |
| Synonyms: | 5-(2,6-Dimorpholinopyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine;NVP-BKM-120;5-(2,6-di-4-morpholinyl-4-pyrimidinyl)-4-(trifluoromethyl)-2-Pyridinamine;BKM120;BKM-120;BKM120 (NVP-BKM120);BKM120 (NVP-BKM120, Buparlisib);Buparlisib（ BKM120, NVP-BKM-120, NVP-BKM120 ）;NVP-BKM 120;NVPBKM120;NVP-BKM-120(5-[2,6-Di(4-morpholinyl)-4-pyrimidinyl]-4-(trifluoromethyl)-2-pyridinamine);Buparlisib;BKM 120;5-[2,6-Di(4-morpholinyl)-4-pyrimidinyl]-4-(trifluoromethyl)-2-pyridinamine;5-[2,6-Di(Morpholin-4-Yl)pyrimidin-4-Yl]-4-(Trifluoromethyl)pyridin-2-Amine;0ZM2Z182GD;AK103313;C18H21F3N6O2;2-Py |
| SMILES: | FC(C1=C([H])C(N([H])[H])=NC([H])=C1C1=C([H])C(=NC(=N1)N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H])N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H])(F)F |
| Formula: | C18H21F3N6O2 |
| M.Wt: | 410.39 |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | NVP-BKM120 is a pan-class I PI3K inhibitor, with IC50s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively. |
| In Vivo: | In A2780 xenograft tumors, oral dosing of NVP-BKM120 (BKM120) at 3, 10, 30, 60, and 100 mg/kg results in a dose dependent modulation of pAKTSer473. Partial inhibition of pAKTSer473 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[1]. Mice receiving NVP-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, NVP-BKM120 treatment significantly prolongs the survival of tumor-bearing mice (P<0.05)[2]. |
| In Vitro: | NVP-BKM120 (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[1]. NVP-BKM120 induces multiple myeloma (MM) cell apoptosis in both dose- and time-dependent manners. NVP-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 NVP-BKM120 and 24-h treatment are chose in in the following experiments if not stated otherwise. NVP-BKM120 treatment results in a dose-dependent growth inhibition in all tested MM cell lines. NVP-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, NVP-BKM120 treatment results in MM cell growth inhibition and apoptosis in dose- and time-dependent manners[2]. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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