GS-9820
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- CAS号:
- 870281-34-8
- 英文名:
- GS-9820
- 英文别名:
- GS-9820;CS-1758;Acalisib;UNII-OVW60IDW1D;Acalisib (GS-9820);Acalisib(GS9820,CAL-120);UNII-OVW60IDW1D;ACALISIB (GS-9820);;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;(S)-2-(1-((9H-Purin-6-yl)amino)ethyl)-6-fluoro-3-phenylquinazolin-4(3H)-one
- 中文名:
- GS-9820
- 中文别名:
- 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
- CBNumber:
- CB92725946
- 分子式:
- C21H16FN7O
- 分子量:
- 401.4
- MOL File:
- 870281-34-8.mol
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GS-9820化学性质
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沸点:
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733.7±70.0 °C(Predicted)
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密度:
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1.50±0.1 g/cm3(Predicted)
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储存条件:
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4°C, protect from light
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溶解度:
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insoluble in H2O; insoluble in EtOH; ≥19.2 mg/mL in DMSO
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形态:
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solid
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酸度系数(pKa):
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10.01±0.10(Predicted)
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颜色:
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White to off-white
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GS-9820性质、用途与生产工艺
Acalisib (GS-9820, CAL-120)是一种具有高度选择性的、有效的p110δ抑制剂，IC50为14 nM。它对p110δ的选择性是对其他I类PI3K酶的选择性的114-400倍，对II类和III类PI3K酶和其他PI3K相关蛋白（包括mTOR和DNA-PK）没有活性。
| Target | Value |
p110δ
()
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14 nM
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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.
GS-9820
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/11/08 | HY-12644 | Acalisib | | 1 mg | 350元 |
| 2024/11/08 | HY-12644 | GS-9820
Acalisib | 870281-34-8 | 5mg | 640元 |
870281-34-8, GS-9820 相关搜索:
- Inhibitors
- 合成有机化合物配体
- 细胞生物学试剂
- 小分子抑制剂，天然产物
- 小分子抑制剂
- 抑制剂
- (S)-2-(1-((9H-嘌呤-6-基)氨基)乙基)-6-氟-3-苯基喹唑啉-4(3H)-酮
- 化合物ACALISIB
- PI3KΔ抑制剂(ACALISIB)
- 870281-34-8
- (S)-2-(1-((9H-Purin-6-yl)amino)ethyl)-6-fluoro-3-phenylquinazolin-4(3H)-one
- GS9820,PI3K,CAL120,Inhibitor,CAL 120,Phosphoinositide 3-kinase,Acalisib,inhibit,GS 9820
- 4(3H)-Quinazolinone, 6-fluoro-3-phenyl-2-[(1S)-1-(9H-purin-6-ylamino)ethyl]-
- CS-1758
- UNII-OVW60IDW1D;ACALISIB (GS-9820);
- UNII-OVW60IDW1D
- 6-fluoro-3-phenyl-2-[(1S)-1-[(9H-purin-6-yl)amino]ethyl]-3,4-dihydroquinazolin-4-one
- 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
- (S)-2-(1-((7H-purin-6-yl)amino)ethyl)-6-fluoro-3-phenylquinazolin-4(3H)-one Acalisib (GS-9820)
- Acalisib
- Acalisib (GS-9820)
- GS-9820