GS-9820
中文名称 | GS-9820 |
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中文同义词 | PI3KΔ抑制剂(ACALISIB);化合物ACALISIB;(S)-2-(1-((9H-嘌呤-6-基)氨基)乙基)-6-氟-3-苯基喹唑啉-4(3H)-酮 |
英文名称 | GS-9820 |
英文同义词 | GS-9820;Acalisib (GS-9820);Acalisib;(S)-2-(1-((7H-purin-6-yl)amino)ethyl)-6-fluoro-3-phenylquinazolin-4(3H)-one Acalisib (GS-9820);6-Fluoro-3-phenyl-2-[(1S)-1-(1H-purin-6-ylamino)ethyl]-4(3H)-quinazolinone;6-Fluoro-3-phenyl-2-[1-(7H-purin-6-ylamino)ethyl]-4(3H)-quinazolinone;Acalisib(GS9820,CAL-120);6-fluoro-3-phenyl-2-[(1S)-1-[(9H-purin-6-yl)amino]ethyl]-3,4-dihydroquinazolin-4-one |
CAS号 | 870281-34-8 |
分子式 | C21H16FN7O |
分子量 | 401.4 |
EINECS号 | 604-604-1 |
相关类别 | 抑制剂;小分子抑制剂;小分子抑制剂,天然产物;细胞生物学试剂;Inhibitors |
Mol文件 | 870281-34-8.mol |
结构式 |
GS-9820 性质
沸点 | 733.7±70.0 °C(Predicted) |
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密度 | 1.50±0.1 g/cm3(Predicted) |
储存条件 | 4°C, protect from light |
溶解度 | 不溶于水;不溶于乙醇; DMSO 中≥19.2 mg/mL |
形态 | 固体 |
酸度系数(pKa) | 10.01±0.10(Predicted) |
颜色 | 白色至米白色 |
Target | Value |
p110δ
() | 14 nM |
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.
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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-12644 | Acalisib | 1 mg | 350元 | |
2024/08/19 | HY-12644 | GS-9820 Acalisib | 870281-34-8 | 5mg | 640元 |