Acalisib (GS-9820),870281-34-8

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产品名称：Acalisib (GS-9820)

产品别名：6-fluoro-3-phenyl-2-[(1S)-1-(7H-purin-6-ylamino)ethyl]quinazolin-4-one

英文别名：CAL-120

靶点：PI3K

CAS：870281-34-8

纯度：0.99

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：Acalisib (GS-9820) is a potent and selective inhibitor of PI3Kδ with IC50 value of 12.7 nM

溶解性：Soluble in DMSO

体外研究：

Acalisib (GS-9820) is more selective for PI3Kδ (IC₅₀=12.7 nM) relative to other PI3K class I enzymes (IC₅₀: PI3Kα, 5,441 nM; PI3Kβ, 3,377 nM; PI3Kγ, 1,389 nM). Acalisib is also 10³-fold more selective against PI3Kδ than against related kinases, such as PI3KCIIβ (IC₅₀>10 nM), hVPS34 (IC₅₀=12.7 μM), DNA-PK (IC₅₀=18.7 μM), and mTOR (IC₅₀>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.

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