生物活性
CAL-101 (GS-1101,Idelalisib)是PI3K的同种型选择性抑制剂，可诱导慢性淋巴细胞性白血病（CLL）细胞凋亡。
Targets
| Target | Value |
| p110δ | IC50: 2.5nM |
| p110γ | IC50: 89nM |
| p110β | IC50: 565nM |
| p110α | IC50: 820nM |
| hVps34 | IC50: 978nM |
| C2β | IC50: >1μM |
| mTOR | IC50: >1μM |
| PIP5Kα | IC50: >1μM |
| PIP5Kβ | IC50: >1μM |
| DNA-PK | IC50: 6.729μM |
化学数据
| 目录号 | A10172 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 415.4 |
| Formula | C22H18FN7O |
| 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. | 870281-82-6 |
| Synonyms | CAL101 |
| SMILES | CC[C@@H](C1=NC2=C(C(=CC=C2)F)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5 |
溶解度
| In vitro (25°C) | DMSO | Warmed: 76 mg/mL (182.94 mM) |
| Water | Insoluble |
| Ethanol | 21 mg/mL (50.55 mM) |
| In vivo | 2% DMSO+20%PEG 300+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 | 24.07 mL | 120.37 mL | 240.73 mL |
| 0.5 mM | 4.81 mL | 24.07 mL | 48.15 mL |
| 1 mM | 2.41 mL | 12.04 mL | 24.07 mL |
| 5 mM | 0.48 mL | 2.41 mL | 4.81 mL |
*The above data is based on the productmolecular weight 415.4 . 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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