生物活性
XL147 analogue是一种有效的，选择性的，口服可生物利用的I类磷脂酰肌醇3激酶（PI3K）小分子抑制剂，作用于PI3Kα/δ/γ，对PI3Kβ作用效果稍弱。具有潜在的抗肿瘤活性。
Targets
| Target | Value |
| PI3Kγ | IC50: 23nM |
| PI3Kδ | IC50: 36nM |
| PI3Kα | IC50: 39nM |
| PI3Kβ | IC50: 383nM |
| DNA-PK | IC50: 4.75μM |
| Vps34 | IC50: 6.975μM |
| MEK | IC50: >10μM |
| B-Raf/C-Raf | IC50: >10μM |
| mTOR | IC50: >15μM |
化学数据
| 目录号 | A10995 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 448.5 |
| Formula | C21H16N6O2S2 |
| 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. | 956958-53-5 |
| Synonyms | XL-147, SAR245408 |
| SMILES | CC1=CC=C(C=C1)S(=O)(=O)NC2=NC3=CC=CC=C3N=C2NC4=CC5=NSN=C5C=C4 |
溶解度
| In vitro (25°C) | DMSO | 3 mg/mL (6.68 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 30% PEG400+0.5% Tween80+5% propylene glycol | 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 | 22.3 mL | 111.48 mL | 222.97 mL |
| 0.5 mM | 4.46 mL | 22.3 mL | 44.59 mL |
| 1 mM | 2.23 mL | 11.15 mL | 22.3 mL |
| 5 mM | 0.45 mL | 2.23 mL | 4.46 mL |
*The above data is based on the productmolecular weight 448.5 . 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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