生物活性
BYL719 (Alpelisib)是一种口服生物可利用的磷脂酰肌醇3-激酶(PI3K)抑制剂，抑制 p110α/p110γ/p110δ/p110β 的 IC50 分别为 5 nM，250 nM，290 nM，1200 nM 。具有潜在的抗肿瘤活性。
靶点信息
| PI3Kα (Cell-free assay) | | | | |
| 5 nM | | | | |
化学数据
| 目录号 | A11328 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 441.5 |
| Formula | C19H22F3N5O2S |
| 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. | 1217486-61-7 |
| Synonyms | BYL-719 |
| SMILES | CC1=C(SC(=N1)NC(=O)N2CCC[C@H]2C(=O)N)C3=CC(=NC=C3)C(C)(C)C(F)(F)F |
溶解度
| In vitro (25°C) | DMSO | 77 mg/mL (174.41 mM) |
| Water | Insoluble |
| Ethanol | 2 mg/mL (4.53 mM) |
| In vivo | 5%DMSO+40%PEG300+5%Tween80+50%ddH2O | 4.1 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 | 22.65 mL | 113.25 mL | 226.5 mL |
| 0.5 mM | 4.53 mL | 22.65 mL | 45.3 mL |
| 1 mM | 2.27 mL | 11.33 mL | 22.65 mL |
| 5 mM | 0.45 mL | 2.27 mL | 4.53 mL |
*The above data is based on the productmolecular weight 441.5 . 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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