生物活性
BKM120 (NVP-BKM120,Buparlisib)是生物可利用的口服泛I类磷脂酰肌醇3激酶（PI3K）激酶抑制剂，在无细胞试验中作用于p110α/β/δ/γ的。对VPS34，mTOR，DNAPK的作用效果下降，而对 PI4Kβ几乎没有活性。
Targets
| Target | Value |
| p110α | IC50: 52nM |
| p110δ | IC50: 116nM |
| p110β | IC50: 166nM |
| p110γ | IC50: 262nM |
| Vps34 | IC50: 2.4μM |
| mTOR | IC50: 4.6μM |
| DNA-PK | IC50: >5μM |
| PI4Kβ | IC50: >25μM |
化学数据
| 目录号 | A11016 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 410.4 |
| Formula | C18H21F3N6O2 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 944396-07-0 |
| SMILES | C1COCCN1C2=NC(=NC(=C2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4 |
溶解度
| In vitro (25°C) | DMSO | 76 mg/mL (185.18 mM) |
| Water | Insoluble |
| Ethanol | 2 mg/mL (4.87 mM) |
| In vivo | 5% DMSO+30% PEG 300+ddH2O | 14 mg/mL |
*<1 mg/ml means slightly soluble or insoluble.
*Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 24.37 mL | 121.83 mL | 243.66 mL |
| 0.5 mM | 4.87 mL | 24.37 mL | 48.73 mL |
| 1 mM | 2.44 mL | 12.18 mL | 24.37 mL |
| 5 mM | 0.49 mL | 2.44 mL | 4.87 mL |
*The above data is based on the productmolecular weight 410.4 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
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