生物活性
GDC-0941 (Pictilisib)是一种强效、选择性、口服生物可利用的I类PI3激酶(PI3K)抑制剂，p110 α、β、δ和γ亚型、DNA-PK和mTOR的IC50值分别为3、33、3、75、1230和580 nM。
Targets
| Target | Value |
| p110α | IC50: 3nM |
| p110δ | IC50: 3nM |
| p110β | IC50: 33nM |
| p110γ | IC50: 75nM |
| mTOR | Kiapp | 0.58μM |
| C2β | IC50: 0.67μM |
| DNA-PK | IC50: 1.23μM |
| Vps34 | IC50: >10μM |
化学数据
| 目录号 | A10421 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 513.6 |
| Formula | C23H27N7O3S2 |
| 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. | 957054-30-7 |
| Synonyms | GDC0941 |
| SMILES | CS(=O)(=O)N1CCN(CC1)CC2=CC3=C(S2)C(=NC(=N3)C4=C5C=NNC5=CC=C4)N6CCOCC6 |
溶解度
| In vitro (25°C) | DMSO | 40 mg/mL (77.87 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 2% DMSO+30% PEG 300+5% Tween 80+ddH2O | 4 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 | 19.47 mL | 97.35 mL | 194.7 mL |
| 0.5 mM | 3.89 mL | 19.47 mL | 38.94 mL |
| 1 mM | 1.95 mL | 9.74 mL | 19.47 mL |
| 5 mM | 0.39 mL | 1.95 mL | 3.89 mL |
*The above data is based on the productmolecular weight 513.6 . 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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