Acalisib
Acalisib(Acalisib)
CAS: 870281-34-8
化学式: C21H16FN7O
| 中文名 | Acalisib |
| 英文名 | Acalisib |
| 别名 | 化合物ACALISIB PI3KΔ抑制剂(ACALISIB) (S)-2-(1-((9H-嘌呤-6-基)氨基)乙基)-6-氟-3-苯基喹唑啉-4(3H)-酮 |
| 英文别名 | GS-9820 Acalisib Acalisib (GS-9820) Acalisib(GS9820,CAL-120) 6-Fluoro-3-phenyl-2-[1-(7H-purin-6-ylamino)ethyl]-4(3H)-quinazolinone 6-Fluoro-3-phenyl-2-[(1S)-1-(1H-purin-6-ylamino)ethyl]-4(3H)-quinazolinone 6-fluoro-3-phenyl-2-[(1S)-1-[(9H-purin-6-yl)amino]ethyl]-3,4-dihydroquinazolin-4-one (S)-2-(1-((7H-purin-6-yl)amino)ethyl)-6-fluoro-3-phenylquinazolin-4(3H)-one Acalisib (GS-9820) |
| CAS | 870281-34-8 |
| EINECS | 604-604-1 |
| 化学式 | C21H16FN7O |
| 分子量 | 401.4 |
| 密度 | 1.50±0.1 g/cm3(Predicted) |
| 沸点 | 733.7±70.0 °C(Predicted) |
| 溶解度 | DMSO: ≥ 29 mg/mL |
| 酸度系数 | 10.01±0.10(Predicted) |
| 存储条件 | -20℃ |
| 体外研究 | Acalisib (GS-9820) is more selective for PI3Kδ (IC 50 =12.7 nM) relative to other PI3K class I enzymes (IC 50 : PI3Kα, 5,441 nM; PI3Kβ, 3,377 nM; PI3Kγ, 1,389 nM). Acalisib is also 10 3 -fold more selective against PI3Kδ than against related kinases, such as PI3KCIIβ (IC 50 >10 nM), hVPS34 (IC 50 =12.7 μM), DNA-PK (IC 50 =18.7 μM), and mTOR (IC 50 >10 nM). In fibroblasts, the PDGF receptor signals through PI3Kα and the GPCR for lysophosphatidic acid (LPA) signals through PI3Kβ. Acalisib reduces PDGF-induced pAkt by only 50% at 11,585 nM, and LPA-induced pAkt by 50% at 2,069 nM. |
| 体内研究 | To dissect the relative contribution of PI3Kα and PI3Kδ inhibition in the reduction of obesity, obese hyperphagic ob/ob mice are treated with a selective PI3Kα inhibitor, BYL-719, or with a selective PI3Kδ inhibitor, Acalisib (GS-9820). Remarkably, BYL-719 reduces body weight after 15 days of treatment to a similar extent as CNIO-PI3Ki, whereas Acalisib has no significant effect at the same doses as BYL-719. It should be noted that 10 mg/kg of Acalisib is sufficient to reduce the growth of multiple myeloma xenografts in mice. |
Acalisib - 配置溶液浓度参考
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.491 ml | 12.457 ml | 24.913 ml |
| 5 mM | 0.498 ml | 2.491 ml | 4.983 ml |
| 10 mM | 0.249 ml | 1.246 ml | 2.491 ml |
| 5 mM | 0.05 ml | 0.249 ml | 0.498 ml |
最后更新：2024-01-02 23:10:35
供应商列表
现货供应
产品名: (S)-2-(1-((9H-嘌呤-6-基)氨基)乙基)-6-氟-3-苯基喹唑啉-4(3H)-酮 去供应商网站查看 询盘CAS: 870281-34-8
产地: 上海
规格: A897452
价格: 5mg-209,10mg-376,25mg-585,50mg-936,100mg-1496,1ml-391
库存: 现货
电话: 13816333479/17821173903
手机: 13816333479/17821173903
电子邮件: wangrui@macklin.cn
QQ: 2885703204/288570320
微信: 19863730987/17821173903
现货供应
产品名: (S)-2-(1-((9H-嘌呤-6-基)氨基)乙基)-6-氟-3-苯基喹唑啉-4(3H)-酮 去供应商网站查看 询盘CAS: 870281-34-8
产地: 上海
规格: A897452
价格: 5mg-209,10mg-376,25mg-585,50mg-936,100mg-1496,1ml-391
库存: 现货
电话: 13816333479/17821173903
手机: 13816333479/17821173903
电子邮件: wangrui@macklin.cn
QQ: 2885703204/288570320
微信: 19863730987/17821173903
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